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Rosiglitazone hydrochloride (Synonyms: BRL 49653 hydrochloride)
Rosiglitazone hydrochloride (BRL 49653 hydrochloride) 是一种选择性的,具有口服活性 PPARγ 激动剂,对 PPARγ1、PPARγ2 和 PPARγ 的 EC50 值分别为 30 nM、100 nM 和 60 nM。Rosiglitazone hydrochloride 与 PPARγ 结合,Kd 约为 40 nM。Rosiglitazone hydrochloride 也是 TRPC5 的激活剂 (EC50=∼30 μM) 和 TRPM3 的抑制剂。
Rosiglitazone hydrochloride Chemical Structure
CAS No. : 302543-62-0
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Rosiglitazone hydrochloride 的其他形式现货产品:
生物活性 |
Rosiglitazone hydrochloride (BRL 49653 hydrochloride) is a selective, orally active PPARγ agonist with EC50s of 30 nM, 100 nM and 60 nM for PPARγ1, PPARγ2, and PPARγ, respectively. Rosiglitazone hydrochloride binds to PPARγ with a Kd of approximately 40 nM. Rosiglitazone hydrochloride is also an activator of TRPC5 (EC50=~30 μM) and an inhibitor of TRPM3[1][2][3][4]. |
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IC50 & Target |
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体外研究 (In Vitro) |
Rosiglitazone is a potent and selective activator of PPARγ, with EC50s of 30 nM and 100 nM for PPARγ1 and PPARγ2, respectively, and a Kd of appr 40 nM for PPARγ. Rosiglitazone (BRL49653, 0.1, 1,10 μM) promotes differentiation of C3H10T1/2 stem cells to adipocytes[1]. Rosiglitazone (Compound 6) activates PPARγ, with an EC50 of 60 nM[2]. Rosiglitazone (1 μM) activates PPARγ, which binds to NF-α1 promoter to activate gene transcription in neurons. Rosiglitazone (1 μM) also protects Neuro2A cells and hippocampal neurons against oxidative stress, and up-regulates BCL-2 expression in an NF-α1-dependent manner[3]. Rosiglitazone completely inhibits TRPM3 with IC50 values of 9.5 and 4.6 μM against nifedipine- and PregS-evoked activity, but such effects are not via PPARγ. Rosiglitazone inhibits TRPM2 at higher concentration, with an IC50 of appr 22.5 μM. Rosiglitazone is a strong stimulator of TRPC5 channels, with an EC50 of ~30 μM[4]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. |
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体内研究 (In Vivo) |
Rosiglitazone (5 mg/kg, p.o.) decreases the serum glucose in diabetic rats. Rosiglitazone also decreases IL-6, TNF-α, and VCAM-1 levels in diabetic group. Rosiglitazone in combination with losartan increases glucose compared to diabetic and Los-treated groups. Rosiglitazone significantly ameliorates endothelial dysfunction indicated by a significantly lower contractile response to PE and Ang II and enhancement of ACh-provoked relaxation in aortas isolated from diabetic rats[5]. Shanghai Jinpan Biotech Co Ltd has not independently confirmed the accuracy of these methods. They are for reference only. |
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Clinical Trial |
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分子量 |
393.89 |
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Formula |
C18H20ClN3O3S |
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CAS 号 |
302543-62-0 |
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中文名称 |
盐酸罗格列酮 |
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运输条件 |
Room temperature in continental US; may vary elsewhere. |
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储存方式 |
Please store the product under the recommended conditions in the Certificate of Analysis. |
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参考文献 |
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