AR-C141990,2250019-94-2

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AR-C141990 hydrochloride

CAS No. : 2250019-94-2

MCE 国际站：AR-C141990 hydrochloride

产品活性：AR-C141990 hydrochloride 是一种有效的乳酸转运蛋白 (monocarboxylate transporters; MCTs) 抑制剂，对 MCT-1 和 MCT-2 的 pK_i 分别为 7.6、6.6。AR-C141990 hydrochloride 具有免疫抑制特性，可抑制移植物抗宿主反应。

研究领域：Membrane Transporter/Ion Channel

作用靶点：Monocarboxylate Transporter

In Vitro: AR-C141990 hydrochloride has no significant activity against MCT-3 (pIC₅₀<5) or MCT-4 (pIC₅₀<5).
AR-C141990 hydrochloride inhibits the uptake of [³H]HOCPCA in oocytes expressing MCT1 or 2 in a concentration-dependent manner with IC₅₀s of 0.21 µM and 2.32 µM, respectively.

In Vivo: AR-C141990 hydrochloride (10 mg/kg; SC) with a parallel decline in plasma concentrations with a half-life around 20 minutes in male NMRI mice (18-22 g) .
Application of the corresponding plasma concentrations of AR-C141990 hydrochloride (0.3-90 mg/kg) results in a concentration-dependent decrease in the B/P of HOCPCA with an EC₅₀ of 860 ng/ml.
AR-C141990 (100 mg/kg; s.c.) has a moderate prolongation of graft survival for 40 days in PVG rats that received DA cardiac transplants.

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