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FXIa-IN-10 (Compound 3f) 是一种有效的激活因子 XI (FXIa) 抑制剂,Ki 值为 0.17 nM。FXIa-IN-10 具有良好的口服生物利用度。

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FXIa-IN-10 Chemical Structure

FXIa-IN-10 Chemical Structure

CAS No. : 2816108-08-2

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Other Forms of FXIa-IN-10:

  • 生物活性

  • 纯度 & 产品资料

  • 参考文献

生物活性

FXIa-IN-10 (Compound 3f) is a potent activated factor XI (FXIa) inhibitor with an Ki of 0.17 nM. FXIa-IN-10 has good oral bioavailability[1].

IC50 & Target

Ki: 0.17 nM (FXIa)[1]

体内研究
(In Vivo)

FXIa-IN-10 (Compound 3f) (1.7+2.0 and 8.5+10.0 (bolus + infusion) mg/kg; i.v.; twice) shows antithrombotic efficacy in a rabbit AV shunt thrombosis model[1].
FXIa-IN-10 (0-10 mg/kg; p.o.; once) demonstrates oral bioavailability in preclinical species (rat 36.4%, dog 80.5%, and monkey 43.0%)[1].

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

Animal Model: Male New Zealand White (NZW) rabbits, AV shunt thrombosis model[1]
Dosage: 1.7+2.0 and 8.5+10.0 (bolus + infusion) mg/kg
Administration: Intravenous injection, 20 min prior to and 40 min during the AV shunt
Result: Reduced thrombus weights in a dose-dependent manner.
Animal Model: Sprague-Dawley rats, Beagle dogs, Cynomolgus monkeys[1]
Dosage: 1, 2, 5 or 10 mg/kg
Administration: Intravenous or oral administration (Pharmacokinetic Analysis)
Result: Pharmacokinetic Profile of FXIa-IN-10 (Compound 3f) in Preclinical Speciesa[1]
animal species clearance (mL/min/kg) T1/2 (h) Vdss (L/kg) F% AUC (iv) (μM•h) AUC (po) (μM•h) Dose iv/po (mpk)
rat 10.7 ± 1.8 1.4 ± 0.0 0.8 ± 0.1 36.4 5.5 ± 1.0 10.0 ± 2.4 2/10
monkey 25.6 ± 4.0 1.0 ± 0.4 1.5 ± 0.4 43.0 1.1 ± 0.2 2.5 ± 0.3 1/5

aCompound was dosed as a free base, vehicle for iv: 20% HPbCD and po: 10% ethanol; 70% PEG-400; 20% water. Data were derived from three animals per study.
分子量

580.35

Formula

C23H18Cl2F3N9O2

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

FXIa-IN-10 相关分类

  • 摩尔计算器

  • 稀释计算器

The molarity calculator equation

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

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The dilution calculator equation

Concentration (start) × Volume (start) = Concentration (final) × Volume (final)

This equation is commonly abbreviated as: C1V1 = C2V2

浓度 (start) × 体积 (start) = 浓度 (final) × 体积 (final)
× = ×
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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.

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产品名称:
FXIa-IN-10
目录号:
HY-151196
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