Pirinixic acid (Synonyms: 匹立尼酸; Wy-14643)

目錄號: HY-16995 純度: 99.80%: FAQs
Data Sheet SDS COA 產品使用指南技術支持

Pirinixic acid (Wy-14643) 是一種有效的 PPARα 激動劑，對鼠的 PPARα 和 PPARγ 的 EC₅₀ 值分別為 0.63 μM, 32 μM，對人的 PPARα，PPARγ 和 PPARδ 的 EC₅₀ 值分別為 5.0 μM，60 μM，35 μM。

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Pirinixic acid Chemical Structure

CAS No. : 50892-23-4

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規(guī)格	價格	是否有貨
10 mM * 1 mL in DMSO	￥550	In-stock
1 mg	￥156	In-stock
5 mg	￥312	In-stock
10 mg	￥500	In-stock
50 mg	￥780	In-stock
100 mg	￥1100	In-stock
250 mg	￥2450	In-stock
500 mg		詢價
1 g		詢價

or 大包裝詢價

* Please select Quantity before adding items.

Customer Review

MCE 顧客使用本產品發(fā)表的 16 篇科研文獻

•Cell Stem Cell. 2022 Sep 1;29(9):1366-1381.e9. [Abstract]
•EBioMedicine. 2024 Mar 19:102:105079. [Abstract]
•Theranostics. 2021 Jan 1;11(5):2247-2262. [Abstract]
•Theranostics. 2020 Feb 18;10(8):3579-3593. [Abstract]
•Environ Pollut. 2021, 117792.
•Biomed Pharmacother. 2024 Jul:176:116837. [Abstract]
•Thromb Res. 2024 Apr 16.
•Acta Physiol. 2023 Apr 25.
•Ecotoxicol Environ Saf. February 2022, 113173.
•iScience. 2023 Nov 9.
•J Inflamm Res. 2022 Aug 22;15:4763-4784. [Abstract]
•J Cell Mol Med. 2021 Dec 28. [Abstract]

•Toxicol Appl Pharmacol. 2024 Jul 25:117042. [Abstract]
•Heliyon. 2023 Aug 19.
•PPAR Res. 2021 Apr 19;2021:6631605. [Abstract]
•BMC Cancer. 2019 Dec 2;19(1):1166. [Abstract]

Pirinixic acid 相關產品

•相關化合物庫:

•同靶點產品:

•同靶點蛋白產品:

查看 PPAR 亞型特異性產品:

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PPARα PPARβ/δ PPARγ PPAR PPARδ

生物活性
實驗參考方法
純度 & 產品資料
參考文獻

生物活性

Pirinixic acid (Wy-14643) is a potent agonist of PPARα, with EC₅₀s of 0.63 μM, 32 μM for murine PPARα and PPARγ, and 5.0 μM, 60 μM, 35 μM for human PPARα, PPARγ and PPARδ, respectively.

IC₅₀ & Target^[1]

PPARα

0.63 μM (EC₅₀)

PPARγ

32 μM (EC₅₀)

細胞效力
(Cellular Effect)

Cell Line	Type	Value	Description	References
COS-7	IC₅₀	36.3 μM Compound: 1	Activation of human PPARalpha ligand binding domain expressed in COS7 cells by luciferase reporter gene assay Activation of human PPARalpha ligand binding domain expressed in COS7 cells by luciferase reporter gene assay	[PMID: 25037914]
COS-7	EC₅₀	39.8 μM Compound: 1, WY-14,643	Agonist activity at wild-type human PPARalpha LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay Agonist activity at wild-type human PPARalpha LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay	[PMID: 25022880]
COS-7	EC₅₀	53.7 μM Compound: 1, WY-14,643	Agonist activity at human PPARgamma LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay Agonist activity at human PPARgamma LBD expressed in COS7 cells after 12 hrs by Dual-Glo luciferase assay	[PMID: 25022880]
COS-7	EC₅₀	53.7 μM Compound: 1	Transactivation of human PPARgamma LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay Transactivation of human PPARgamma LBD expressed in african green monkey Cos7 cells co-transfected with fused GAL4-DBD after 14 hrs by Dual-Glo Luciferase reporter gene assay	[PMID: 20307981]
COS-7	IC₅₀	53.7 μM Compound: 1	Activation of human PPARgamma ligand binding domain expressed in COS7 cells by luciferase reporter gene assay Activation of human PPARgamma ligand binding domain expressed in COS7 cells by luciferase reporter gene assay	[PMID: 25037914]
CV-1	EC₅₀	0.13 μM Compound: Wy14643	Transactivation of human PPARalpha expressed in african green monkey CV1 cells by luciferase reporter gene assay Transactivation of human PPARalpha expressed in african green monkey CV1 cells by luciferase reporter gene assay	[PMID: 22579420]
HEK293	EC₅₀	23.33 μM Compound: WY-14643	Agonist activity at human PPARalpha expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay Agonist activity at human PPARalpha expressed in HEK293 cells cotransfected with PPREx4-TK-luc assessed as activation of luciferase activity measured after 48 hrs by transactivation assay	[PMID: 23265844]
HepG2	EC₅₀	0.04 μM Compound: WY-14643	Agonist activity at mouse PPARalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay Agonist activity at mouse PPARalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay	[PMID: 19053776]
HepG2	EC₅₀	1.56 μM Compound: Wy 14,643	Transactivation of GAL4-fused human PPARalpha ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay Transactivation of GAL4-fused human PPARalpha ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene assay	[PMID: 23171045]
HepG2	EC₅₀	1.56 μM Compound: Wy-14,643	Agonist activity at human GAL4-PPARalpha ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay Agonist activity at human GAL4-PPARalpha ligand binding domain expressed in human HepG2 cells by luciferase reporter gene assay	[PMID: 25462281]
HepG2	EC₅₀	1.6 μM Compound: Wy-14,643	Agonist activity at GAL4-tagged human PPARalpha ligand binding domain expressed in HepG2 cells assessed as transactivation after 20 hrs by beta-galactosidase reporter gene assay Agonist activity at GAL4-tagged human PPARalpha ligand binding domain expressed in HepG2 cells assessed as transactivation after 20 hrs by beta-galactosidase reporter gene assay	[PMID: 22341573]
HepG2	EC₅₀	1.6 μM Compound: WY-14643	Agonist activity at human GAL4-fused PPARalpha ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivation assay Agonist activity at human GAL4-fused PPARalpha ligand binding domain expressed in HepG2 cells after 20 hrs by luciferase reporter gene transactivation assay	[PMID: 22081932]
HepG2	EC₅₀	1.6 μM Compound: WY-14643	Agonist activity at GAL4-tagged human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay Agonist activity at GAL4-tagged human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation by luciferase reporter gene assay	[PMID: 19775169]
HepG2	EC₅₀	1.6 μM Compound: WY-14643	Agonist activity at human PPARgamma ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay Agonist activity at human PPARgamma ligand binding domain expressed in human HepG2 cells co-transfected with Gal4 by luciferase reporter gene assay	[PMID: 18835719]
HepG2	EC₅₀	1.62 μM Compound: Wy-14,643	Agonist activity at GAL4-DNA binding domain fused human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay Agonist activity at GAL4-DNA binding domain fused human PPARalpha ligand binding domain expressed in human HepG2 cells assessed as receptor transactivation incubated for 20 hrs by luciferase reporter gene assay	[PMID: 25497132]
HepG2	EC₅₀	1.62 μM Compound: WY-14643	Agonist activity at human PPARalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay Agonist activity at human PPARalpha ligand binding domain expressed in human Hep G2 cells co-transfected with Gal4-DBD by luciferase reporter gene assay	[PMID: 19053776]
HepG2	EC₅₀	3.46 μM Compound: WY14643	Agonist activity at GAL4-fused PPARalpha (unknown origin) expressed in human HepG2 cells by transactivation assay Agonist activity at GAL4-fused PPARalpha (unknown origin) expressed in human HepG2 cells by transactivation assay	[PMID: 23502212]
HepG2	EC₅₀	4.8 μM Compound: WY-14643	Agonist activity at PPARalpha expressed in human HepG2 cells assessed as induction of receptor transactivation by reporter gene assay relative to control Agonist activity at PPARalpha expressed in human HepG2 cells assessed as induction of receptor transactivation by reporter gene assay relative to control	[PMID: 18625559]
HepG2	EC₅₀	4800 nM Compound: WY-14643	Transactivation of human PPARalpha expressed in human HepG2 cells co-transfected with PPRE3-TK-Luc by luciferase reporter gene assay Transactivation of human PPARalpha expressed in human HepG2 cells co-transfected with PPRE3-TK-Luc by luciferase reporter gene assay	[PMID: 21450468]
HepG2	EC₅₀	7.1 μM Compound: WY14643	Agonist activity at GAL4-fused PPARalpha A454M mutant (unknown origin) expressed in human HepG2 cells by transactivation assay Agonist activity at GAL4-fused PPARalpha A454M mutant (unknown origin) expressed in human HepG2 cells by transactivation assay	[PMID: 23502212]
MCF7	EC₅₀	542 nM Compound: WY-14643	Agonist activity at human PPARalpha expressed in MCF7 cells co-transfected CPTI DR1-type RE after 6 hrs by luciferase reporter gene assay Agonist activity at human PPARalpha expressed in MCF7 cells co-transfected CPTI DR1-type RE after 6 hrs by luciferase reporter gene assay	[PMID: 24936232]
MCF7	EC₅₀	650 nM Compound: WY-14643	Agonist activity at human PPARalpha expressed in MCF7 cells co-transfected CPTI DR1-type RE after 16 hrs by luciferase reporter gene assay Agonist activity at human PPARalpha expressed in MCF7 cells co-transfected CPTI DR1-type RE after 16 hrs by luciferase reporter gene assay	[PMID: 24936232]
U2OS	EC₅₀	12 μM Compound: WY-14643	Agonist activity at human PPARalpha in U2OS cells by transactivation assay Agonist activity at human PPARalpha in U2OS cells by transactivation assay	[PMID: 18329751]

體外研究
(In Vitro)

Pirinixic acid (Wy-14643) 是 PPARα 的激動劑，小鼠 PPARα 和 PPARγ 的 EC₅₀ 為 0.63 μM，32 μM，人 PPARα，PPARγ 為 5.0 μM，60 μM，35 μM和 PPARδ^[1]。
Pirinixic acid (Wy-14643；0，10，100 μM) 增強滑膜成纖維細胞中 PPAR-α 的蛋白表達。Pirinixic acid (0，10，100 μM) 對 LPS 刺激的滑膜成纖維細胞中的 NO 和 PGE2 產生有抑制作用。Pirinixic acid 還有效下調滑膜成纖維細胞中炎癥介質如 VCAM-1、ICAM-1、ET-1 和 TF 的表達，阻斷滑膜成纖維細胞中 LPS 誘導的 NF-kB 活化、IkB 磷酸化和 NF-kB 核轉位，但 Pirinixic acid 對 PPAR-α 沉默的細胞沒有影響^[2]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

體內研究
(In Vivo)

Pirinixic acid (Wy-14643；10 mg/kg，iv) 降低肥胖大鼠的肝損傷和脂質過氧化 (MDA) 水平。Pirinixic acid 還會導致 Sham 和缺血再灌注 (IR) 組的 SIRT1 活性增加，但對 SIRT3 蛋白表達沒有影響。Pirinixic acid 可提高大鼠的 NAD⁺ 和 ATP 水平，并防止內質網應激 (ERS)^[3]。

MCE has not independently confirmed the accuracy of these methods. They are for reference only.

分子量

323.80

Formula

C₁₄H₁₄ClN₃O₂S

CAS 號

50892-23-4

性狀

固體

顏色

White to off-white

運輸條件

Room temperature in continental US; may vary elsewhere.

儲存方式

Powder	-20°C	3 years
	4°C	2 years
In solvent	-80°C	2 years
	-20°C	1 year

溶解性數(shù)據(jù)

細胞實驗：

DMSO 中的溶解度 : 100 mg/mL (308.83 mM; 超聲助溶; 吸濕的 DMSO 對產品的溶解度有顯著影響，請使用新開封的 DMSO)

H₂O 中的溶解度 : < 0.1 mg/mL (insoluble)

配制儲備液

濃度溶劑體積質量	1 mg	5 mg	10 mg

1 mM	3.0883 mL	15.4416 mL	30.8833 mL
5 mM	0.6177 mL	3.0883 mL	6.1767 mL
10 mM	0.3088 mL	1.5442 mL	3.0883 mL

查看完整儲備液配制表

* 請根據(jù)產品在不同溶劑中的溶解度選擇合適的溶劑配制儲備液；一旦配成溶液，請分裝保存，避免反復凍融造成的產品失效。
儲備液的保存方式和期限：-80°C, 2 years; -20°C, 1 year。-80°C儲存時，請在2年內使用， -20°C儲存時，請在1年內使用。

摩爾計算器
稀釋計算器

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Concentration _(start) × Volume _(start) = Concentration _(final) × Volume _(final)

This equation is commonly abbreviated as: C₁V₁ = C₂V₂

濃度 _(start)

體積 _(start)

濃度 _(final)

體積 _(final)

動物實驗：

請根據(jù)您的實驗動物和給藥方式選擇適當?shù)娜芙夥桨浮?

以下溶解方案都請先按照 In Vitro 方式配制澄清的儲備液，再依次添加助溶劑：
——為保證實驗結果的可靠性，澄清的儲備液可以根據(jù)儲存條件，適當保存；體內實驗的工作液，建議您現(xiàn)用現(xiàn)配，當天使用；
以下溶劑前顯示的百分比是指該溶劑在您配制終溶液中的體積占比；如在配制過程中出現(xiàn)沉淀、析出現(xiàn)象，可以通過加熱和/或超聲的方式助溶

方案一

請依序添加每種溶劑： 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: 10 mg/mL (30.88 mM); 懸濁液; 超聲助溶

此方案可獲得 10 mg/mL的均勻懸濁液，懸濁液可用于口服和腹腔注射。
以 1 mL 工作液為例，取 100 μL 100.0 mg/mL 的澄清 DMSO 儲備液加到 400 μL PEG300 中，混合均勻；再向上述體系中加入 50 μL Tween-80，混合均勻；然后再繼續(xù)加入 450 μL 生理鹽水定容至 1 mL。
生理鹽水的配制：將 0.9 g 氯化鈉，溶解于 ddH?O 并定容至 100 mL，可以得到澄清透明的生理鹽水溶液。
方案二

請依序添加每種溶劑： 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (6.42 mM); 澄清溶液

此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液。
以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 900 μL 20% 的 SBE-β-CD 生理鹽水水溶液中，混合均勻。
2 g SBE-β-CD（磺丁基醚 β-環(huán)糊精）粉末定容于 10 mL 的生理鹽水中，完全溶解至澄清透明。
方案三

請依序添加每種溶劑： 10% DMSO 90% Corn Oil
Solubility: ≥ 2.08 mg/mL (6.42 mM); 澄清溶液

此方案可獲得 ≥ 2.08 mg/mL（飽和度未知）的澄清溶液，此方案實驗周期在半個月以上的動物實驗酌情使用。
以 1 mL 工作液為例，取 100 μL 20.8 mg/mL 的澄清 DMSO 儲備液加到 900 μL玉米油中，混合均勻。

動物溶解方案計算器

請輸入動物實驗的基本信息：

給藥劑量

mg/kg

動物的平均體重

每只動物的給藥體積

μL

動物數(shù)量

只

由于實驗過程有損耗，建議您多配一只動物的量

請輸入您的動物體內配方組成：

DMSO +

Tween-80 +

Saline

如果您的動物是免疫缺陷鼠或者體弱鼠，建議 DMSO 中的在最后工作液體系中的占比盡量不超過 2%。

方案所需 助溶劑 包括：DMSO，，均可在 MCE 網站選購。，Tween 80，均可在 MCE 網站選購。

計算結果

工作液所需濃度 : mg/mL

儲備液配制方法 : mg 藥物溶于 μL DMSO（母液濃度為 mg/mL）。

您所需的儲備液濃度超過該產品的實測溶解度，以下方案僅供參考，如有需要，請與 MCE 中國技術支持聯(lián)系。

動物實驗體內工作液的配制方法 : 取 μL DMSO 儲備液，加入 μL 。 μL ，混合均勻至澄清，再加 μL Tween 80，混合均勻至澄清，再加 μL 生理鹽水。

連續(xù)給藥周期超過半月以上，請謹慎選擇該方案。

請確保第一步儲備液溶解至澄清狀態(tài)，從左到右依次添加助溶劑。您可采用超聲加熱（超聲清洗儀，建議頻次 20-40 kHz），渦旋吹打等方式輔助溶解。

純度 & 產品資料

純度: 99.80%

選擇批次：

Data Sheet (644 KB) SDS (418 KB)

COA (284 KB) LCMS (258 KB)

產品使用指南 (1538 KB)

參考文獻

[1]. Willson TM, et al. The PPARs: from orphan receptors to drug discovery. J Med Chem. 2000 Feb 24;43(4):527-50. [Content Brief]

[2]. Huang D, et al. PPAR-α Agonist WY-14643 Inhibits LPS-Induced Inflammation in Synovial Fibroblasts via NF-kB Pathway. J Mol Neurosci. 2016 Aug;59(4):544-53. [Content Brief]

[3]. Pantazi E, et al. PPARα Agonist WY-14643 Induces SIRT1 Activity in Rat Fatty Liver Ischemia-Reperfusion Injury. Biomed Res Int. 2015;2015:894679. [Content Brief]

Cell Assay ^[2]	Synovial fibroblasts are treated with LPS (100 μg/mL) in the presence or absence of Pirinixic acid. PPAR-α siRNA-transfected cells are also treated with LPS (100 μg/mL) together with Pirinixic acid. After stimulation, the production of NO is determined using Griess reagents. Briefly, 300 μL of supernatant is mixed with 100 μL of Griess reagent and 2.6 mL of deionized water. The mixture is incubated for 30 min at room temperature, and the absorbance at 548 nm is measured. The concentrations of NO in the supernatants are calculated from a standard curve^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Animal Administration ^[2]	Synovial fibroblasts are treated with LPS (100 μg/mL) in the presence or absence of Wy-14643. PPAR-α siRNA-transfected cells are also treated with LPS (100 μg/mL) together with Wy-14643. After stimulation, the production of NO is determined using Griess reagents. Briefly, 300 μL of supernatant is mixed with 100 μL of Griess reagent and 2.6 mL of deionized water. The mixture is incubated for 30 min at room temperature, and the absorbance at 548 nm is measured. The concentrations of NO in the supernatants are calculated from a standard curve^[2]. MCE has not independently confirmed the accuracy of these methods. They are for reference only.
參考文獻	[1]. Willson TM, et al. The PPARs: from orphan receptors to drug discovery. J Med Chem. 2000 Feb 24;43(4):527-50. [Content Brief] [2]. Huang D, et al. PPAR-α Agonist WY-14643 Inhibits LPS-Induced Inflammation in Synovial Fibroblasts via NF-kB Pathway. J Mol Neurosci. 2016 Aug;59(4):544-53. [Content Brief] [3]. Pantazi E, et al. PPARα Agonist WY-14643 Induces SIRT1 Activity in Rat Fatty Liver Ischemia-Reperfusion Injury. Biomed Res Int. 2015;2015:894679. [Content Brief]

Pirinixic acid 相關分類

Metabolic Disease Inflammation/Immunology

完整儲備液配制表

可選溶劑	濃度溶劑體積質量	1 mg	5 mg	10 mg	25 mg

DMSO	1 mM	3.0883 mL	15.4416 mL	30.8833 mL	77.2082 mL
	5 mM	0.6177 mL	3.0883 mL	6.1767 mL	15.4416 mL
	10 mM	0.3088 mL	1.5442 mL	3.0883 mL	7.7208 mL
	15 mM	0.2059 mL	1.0294 mL	2.0589 mL	5.1472 mL
	20 mM	0.1544 mL	0.7721 mL	1.5442 mL	3.8604 mL
	25 mM	0.1235 mL	0.6177 mL	1.2353 mL	3.0883 mL
	30 mM	0.1029 mL	0.5147 mL	1.0294 mL	2.5736 mL
	40 mM	0.0772 mL	0.3860 mL	0.7721 mL	1.9302 mL
	50 mM	0.0618 mL	0.3088 mL	0.6177 mL	1.5442 mL
	60 mM	0.0515 mL	0.2574 mL	0.5147 mL	1.2868 mL
	80 mM	0.0386 mL	0.1930 mL	0.3860 mL	0.9651 mL
	100 mM	0.0309 mL	0.1544 mL	0.3088 mL	0.7721 mL

Help & FAQs

Do most proteins show cross-species activity?
Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

Pirinixic acid50892-23-4Wy-14643Wy14643Wy 14643PPARPeroxisome proliferator-activated receptorsInhibitorinhibitorinhibit

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Pirinixic acid (Synonyms: 匹立尼酸; Wy-14643)

Customer Review

MCE 顧客使用本產品發(fā)表的 16 篇科研文獻

Pirinixic acid 相關產品

•相關化合物庫:

•同靶點產品:

•同靶點蛋白產品:

查看 PPAR 亞型特異性產品:

生物活性

實驗參考方法

純度 & 產品資料

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Pirinixic acid (Synonyms: 匹立尼酸; Wy-14643)

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