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| 中文名称 |
SCH 546738
|
|---|---|
| 中文别名 |
3-氨基-6-氯-5-[(3S)-4-[1-[(4-氯苯基)甲基]-4-哌啶基]-3-乙基-1-哌…;3-氨基-6-氯-5-[(3S)-4-[1-[(4-氯苯基)甲基]-4-哌啶基]-3-乙基-1-哌嗪基]-2-哌嗪甲酰胺
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| 英文名称 |
SCH 546738
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| 英文别名 |
(S)-3-Amino-6-chloro-5-(4-(1-(4-chlorobenzyl)piperidin-4-yl)-3-ethylpiperazin-1-yl)pyrazine-2-carboxamide;2-Pyrazinecarboxamide, 3-amino-6-chloro-5-[(3S)-4-[1-[(4-chlorophenyl)methyl]-4-piperidinyl]-3-ethyl-1-piperazinyl]-;3-amino-6-chloro-5-[(3S)-4-[1-[(4-chlorophenyl)methyl]piperidin-4-yl]-3-ethylpiperazin-1-yl]pyrazine-2-carboxamide;PYRAZINECARBOXAMIDE, 3-AMINO-6-CHLORO-5-[(3S)-4-[1-[(4-CHLOROPHENYL)METHYL]-4-PIPERIDINYL]-3-ETHYL-1-PIPERAZINYL]- (9CI);SCH546738;SCH-546738;3-Amino-6-chloro-5-[(3S)-4-[1-[(4-chlorophenyl)methyl]-4-piperidinyl]-3-ethyl-1-piperazinyl]-2-pyrazinecarboxamide (ACI);Pyrazinecarboxamide, 3-amino-6-chloro-5-[(3S)-4-[1-[(4-chlorophenyl)methyl]-4-piperidinyl]-3-ethyl-1-piperazinyl]- (9CI);3-Amino-6-chloro-5-[(3S)-4-[1-[(4-chlorophenyl)methyl]piperidin-4-yl]-3-ethylpiperazin-1-yl]pyrazine-2-carboxamide;SCH 546738
|
| Cas No. |
906805-42-3
|
| 分子式 |
C23H31Cl2N7O
|
| 分子量 |
492.44
|
| 包装储存 |
Powder -20°C 3 years；4°C 2 years
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| 产品详情 |
SCH 546738 是一种有效、可口服的非竞争性 CXCR3 拮抗剂，结合到人 CXCR3 受体的亲和常数 (Ki) 为 0.4 nM。
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|---|---|
| 生物活性 |
SCH 546738 is a potent, orally active and non-competitive CXCR3 antagonist, the affinity constant (K i ) of SCH 546738 binding to human CXCR3 receptor is determined to be 0.4 nM in multiple experiments.
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| 性状 |
Solid
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| IC50 & Target[1][2] |
Human CXCR3 0.4 nM (Ki)
|
| 体外研究(In Vitro) |
The affinity of SCH 546738 binding to human CXCR3 receptor is determined by competition binding analysis using S radiolabeled SCH 535390 (a sulfonamide analog of the CXCR3 compound series with a Kd of 0.6 nM) as a competitive tracer. In addition, SCH 546738 displaces radiolabeled CXCL10 and CXCL11 from human CXCR3 with IC50 ranging from 0.8 to 2.2 nM in a non-competitive manner. SCH 546738 potently and specifically inhibits CXCR3-mediated chemotaxis in human activated T cells with IC90 about 10 nM. Competition of human CXCL10 and CXCL11 binding to human CXCR3 by SCH 546738 is determined at various concentrations of [I]hCXCL10 and [I]hCXCL11 around the Kd (50-100 pM) for the receptor. The IC50 of SCH 546738 is constant (~1 or 2 nM) and independent of the input concentrations of either [I]hCXCL10 (25-500 pM) or [I]hCXCL11 (1
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| 体内研究(In Vivo) |
SCH 546738 has strong cross-species activities with IC 50 of 1.3 nM, 6.4 nM, 5.9 nM and 4.2 nM in inhibiting the binding of [I]hCXCL10 to CXCR3 of monkey, dog, mouse and rat origin, respectively. SCH 546738 is a selective and potent CXCR3 antagonist with a good PK for in vivo studies. In addition, SCH 546738 has a favourable pharmacokinetic profile in rodents, the plasma concentrations of SCH 546738 in Lewis rat and C57BL/6 mouse over 24 hr post-dose. The AUC (0-24 hr) is 7.7 μM.hr in Lewis rat 10 mg/kg (mpk) and is 12.6 μM.hr in C57BL/6 mouse 30 mpk. has not independently confirmed the accuracy of these methods. They are for reference only.
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| 运输条件 |
Room temperature in continental US; may vary elsewhere.
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| 储存方式 |
Powder -20°C 3 years；4°C 2 years
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| 参考文献 |
[1]. Jenh CH, et al. A selective and potent CXCR3 antagonist SCH 546738 attenuates the development of autoimmune diseases and delays graft rejection. BMC Immunol. 2012 Jan 10;13:2.[2]. Zhang X, et al. CXC chemokine receptor 3 promotes steatohepatitis in mice through mediating inflammatory cytokines, macrophages and autophagy. J Hepatol. 2016 Jan;64(1):160-70.
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| 溶解度数据 |
In Vitro: DMSO : 4.5 mg/mL (9.14 mM; Need ultrasonic)H2O : < 0.1 mg/mL (insoluble)配制储备液
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1：一般建议：溶解度为Medlife测试数据，可能与文献描述存在差异。这是由于生产工艺和批次不同产生的正常现象。为了使其更好的溶解，请用37℃加热试管并在超声波水浴中震动片刻。不同批次产品溶解度各有差异，仅做参考，具体以实验方案为准。
2：储存条件：粉末-20°C一般情况可以保存3年，溶于溶剂-80°C一般情况可以保存1年。不同产品及不同批次产品可能存在差异，请细致阅读产品信息，并辅助参考相关文献描述。
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