2. GPCR/G Protein Immunology/Inflammation Anti-infection
  3. CCR HIV
  4. CCR5 antagonist 2

CCR5 antagonist 2 (Compound 25) 是一种 CCR5 拮抗剂，其 IC50 为 8.34 nM。CCR5 antagonist 2 显示广谱抗 HIV-1 活性。

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CCR5 antagonist 2 Chemical Structure

CCR5 antagonist 2 Chemical Structure

CAS No. : 1800570-93-7

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CCR5 antagonist 2 相关抗体

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CCR1 CCR2 CCR3 CCR4 CCR5 CCR6 CCR7 CCR8 CCR9

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  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

CCR5 antagonist 2 (Compound 25) is a CCR5 antagonist with an IC50 of 8.34 nM. CCR5 antagonist 2 shows broad-spectrum anti-HIV-1 activities[1].

IC50 & Target[1]

CCR5

8.34 nM (IC50)

HIV-1

11 nM (EC50, TZM-bl cell)

体外研究
(In Vitro)

CCR5 antagonist 2 (Compound 25) (48 h) 在 TZM-bl 细胞中表现出优异的 HIV-1 抑制活性，EC50 为 0.011 ± 0.002 μM[1]。
CCR5 antagonist 2 (48 h) 对 TZM-bl 细胞中亲 CCR5 整合酶抑制剂耐药株 HIV-1YU-2(G140S/Q148H) 具有抗病毒活性，EC50 为 4.34 ± 1.61 nM[1]。
CCR5 antagonist 2 对 HIV-1 菌株 KIZ001、YU-2、KIZ006、SF162 和 Ba-L 有抑制作用，EC50 分别为 7.82、8.73、12.61、15.99 和 16.93 nM[1]。

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

CCR5 antagonist 2 相关抗体:
体内研究
(In Vivo)

PK Properties of CCR5 antagonist 2 (Compound 25) in SD Rats[1]

compd admin dose (mg/kg) Cmax (ng/mL) Tmax (h) T1/2 (h) AUC0–last (ng·h/mL) AUC0–∞ (ng·h/mL) MRT (h) CL (mL/min/kg) F (%)
CCR5 antagonist 2 p.o. 10 49.5 ± 18.6 2.0 ± 0.0 10.3 ± 2.5 229 ± 92 283 ± 105 13.2 ± 4.2 – 15.7
i.v. 2 – – 1.60 ± 0.03 291 ± 75 298 ± 76 1.81 ± 0.04 117 ± 29

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

Animal Model: SD rats[1]
Dosage: 2 mg/kg and 10 mg/kg
Administration: Intravenous and oral administration (Pharmacokinetic Analysis)
Result: Displayed good PK profiles.
分子量

601.79

Formula

C32H45F2N5O2S
CAS 号
运输条件

Room temperature in continental US; may vary elsewhere.
储存方式

Please store the product under the recommended conditions in the Certificate of Analysis.
纯度 & 产品资料
参考文献

CCR5 antagonist 2 相关分类

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  • 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:

CCR5 antagonist 21800570-93-7CCRHIVCC chemokine receptorHuman immunodeficiency virusKIZ001YU-2KIZ006SF162Ba-LTZM-blPBMCsInhibitorinhibitorinhibit

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