2. Anti-infection Membrane Transporter/Ion Channel Metabolic Enzyme/Protease
  3. Reverse Transcriptase HIV Potassium Channel Cytochrome P450
  4. NNRT-IN-10

NNRT-IN-10 是一种强效，有选择性且口服有效的非核苷类 HIV-1 逆转录酶抑制剂 (NNRTI)。NNRT-IN-10 对 HIV 和其突变株的 EC50 值范围在 1.16 至 18.3 nM之间。NNRT-IN-10 具有良好的药代动力学特性和安全性。NNRT-IN-10 可用于研究由 HIV-1 引发的艾滋病。

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NNRT-IN-10

NNRT-IN-10 Chemical Structure

CAS No. : 2459751-62-1

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NNRT-IN-10 相关抗体

Top Publications Citing Use of Products

查看 HIV 亚型特异性产品:

查看所有亚型
HIV HIV-1 HIV-2

查看 Cytochrome P450 亚型特异性产品:

查看所有亚型
CYP1 CYP2 CYP3 CYP4 CYP11 CYP17 Aromatase/CYP19A1 CYP26 CYP51 CYP1A2 CYP2D6 CYP2C9 CYP2C19 CYP3A4 CYP17A1

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

NNRT-IN-10 is a potent, selective and orally active non-nucleoside HIV-1 reverse transcriptase (NNRTI) inhibitor with with an EC50 values ranging from 1.16 to 18.3 nM for HIV and its mutant strains. NNRT-IN-10 exhibits good pharmacokinetic properties and favorable safety profiles. NNRT-IN-10 can be used for the study of AIDS, caused by HIV-1[1].

IC50 & Target[1]

HIV-1 (WT)

1.16 nM (EC50)

CYP1A2

56.6 μM (IC50)

CYP2C9

6.76 μM (IC50)

CYP2C19

8.47 μM (IC50)

CYP2D6

12.7 μM (IC50)

体外研究
(In Vitro)

NNRT-IN-10 (Compound 5i3) (48 h) 具有改良的抗药性且无明显的细胞毒性，其 EC50 值分别为：1.16 nM (HIV-1, WT)、2.64 nM (P1579)、12.5 nM (P5375)、3.70 nM (P1833) 和 18.3 nM (P5735)[1]。
NNRT-IN-10 (5 d) 在 MT-4 细胞中，纳摩尔水平 (EC50 = 1.4 nM) 下能非常有效地抑制 HIV-1 IIIB 的复制[1]。
NNRT-IN-10 对 CYP1A2 (IC50 = 56.6 μM)、CYP2C9 (IC50 = 6.76 μM)、CYP2C19 (IC50 = 8.47 μM) 和 CYP2D6 (IC50 = 12.7 μM) 仅表现出轻微的抑制作用[1]。
NNRT-IN-10 (0.3-40 μM, 24 h) 在 CHO-hERG 细胞中显示出对钾离子通道的抑制活性，其 IC50 值为 1.48 μM[1]。

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

NNRT-IN-10 相关抗体:
药代动力学
(Parmacokinetics)
Species Dose Route Indicator value
Rat 20 mg/kg p.o. F 59.9 %
Rat 2 mg/kg i.v. CL 20.6 mL/min/kg
Rat 2 mg/kg i.v. T1/2 1.59 h
Rat 20 mg/kg p.o. T1/2 1.77 h
Rat 20 mg/kg p.o. Tmax 0.417 h
Rat 2 mg/kg i.v. AUC0-inf 1675 ng·h/mL
Rat 20 mg/kg p.o. MRT0-inf 3.48 h
Rat 2 mg/kg i.v. AUC0-last 1661 ng·h/mL
Rat 2 mg/kg i.v. Vd 1513 mL/kg
Rat 20 mg/kg p.o. AUC0-inf 10033 ng·h/mL
Rat 2 mg/kg i.v. MRT0-last 1.17 h
Rat 20 mg/kg p.o. AUC0-last 9934 ng·h/mL
Rat 20 mg/kg p.o. MRT0-last 3.37 h
Rat 2 mg/kg i.v. MRT0-inf 1.25 h
Rat 20 mg/kg p.o. Cmax 2354 ng/mL
体内研究
(In Vivo)

NNRT-IN-10 (Compound 5i3) (800 mg/kg, p.o., 单剂量) 耐受性良好，对小鼠无急性毒性[1]。

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

568.69

Formula

C31H32N6O3S
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

NNRT-IN-10 相关分类

  • 摩尔计算器

  • 稀释计算器

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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:

NNRT-IN-102459751-62-1Reverse TranscriptaseHIVPotassium ChannelCytochrome P450Human immunodeficiency virusKcsACYPsHIV-1antiretroviral therapynon-nucleoside reverse-transcriptasedrug resistancepharmacokineticsInhibitorinhibitorinhibit

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