2. Metabolic Enzyme/Protease
  3. Factor Xa
  4. FXIa-IN-8

FXIa-IN-8 是一种有效的选择性 FXIa 抑制剂， IC50 为 14.2 nM。FXIa-IN-8 具有抗血栓形成活性，且不会增加出血风险和明显的毒性sup>[1]。

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FXIa-IN-8 Chemical Structure

FXIa-IN-8 Chemical Structure

CAS No. : 2744293-04-5

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FXIa-IN-8 相关抗体

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  • 生物活性

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  • 参考文献

生物活性

FXIa-IN-8 is a potent and selective FXIa inhibitor with an IC50 of 14.2 nM. FXIa-IN-8 shows antithrombotic activity without increasing the bleeding risk and obvious toxicitysup>[1].

IC50 & Target

IC50: 14.2 nM (FXIa); 27900 nM (PKal)[1]
体外研究
(In Vitro)

FXIa-IN-8 (compound 35) (0-250 µg/mL) shows significant anticoagulant activity toward the intrinsic pathway without affecting the extrinsic pathway[1].

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

FXIa-IN-8 相关抗体:
体内研究
(In Vivo)

FXIa-IN-8 shows selectivity for FXIa and PKal with IC50s of 14.2, 27900 nM, respectively[1].
FXIa-IN-8 (6.5, 19.5 mg/kg; i.v.) shows antithrombotic activity in vivo[1].
FXIa-IN-8 (50, 100 mg/kg; i.v.) shows no acute toxicity[1].
FXIa-IN-8 (10 mg/kg; i.v.) shows moderate PK profiles[1]. FXIa-IN-8 (19.5, 39 mg/kg) exhibits a much lower bleeding risk than heparin sodium at 300 IU/kg[1].
Pharmacokinetic Parameters of FXIa-IN-8 in Male SD rats[1].

compd 35 T1/2 (h) Cmax (µg/mL) AUC0-t (h·µg/mL) AUC0-∞ (h·µg/mL) Vz(mL/kg) Cl (mL/h/kg) MRT0-t (h)
i.v. (10 mg/kg) 1.26 57 18.3 18.4 969 553 0.32
Male SD rats; 10 mg/kg for i.v.[1].

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

Animal Model: Male SD rats[1]
Dosage: 10 mg/kg (300 IU/kg (2.7 mg/kg) heparin sodium were injected into the tail vein 10 min before surgery)
Administration: I.v.
Result: Showed moderate PK profiles with a half-life value (T1/2) of 1.26 h and a clearance (Cl) value of 553 mL/h/kg.
Animal Model: C57BL/6J mice (FeCl3-induced carotid artery thrombus model)[1]
Dosage: 6.5, 19.5 mg/kg
Administration: I.v.
Result: Slightly prolonged the time of occlusion at 6.5 mg/kg, and showed excellent antithrombotic activity at 35 mg/kg.
Animal Model: ICR mice[1]
Dosage: 50, 100 mg/kg
Administration: I.v.
Result: Showed no obvious toxic reaction to different tissues of mice.
Animal Model: C57BL/6J mice[1]
Dosage: 19.5, 39, 20, 60, 100 mg/kg
Administration: I.v.
Result: Showed a low bleeding risk at 60 and 100 mg/kg.
分子量

629.07

Formula

C31H29ClN8O5
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-8 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:

FXIa-IN-82744293-04-5Factor XaFxaAntithromboticICR miceacute toxicitybleeding riskSD ratsFeCl3-induced carotid artery thrombus modelInhibitorinhibitorinhibit

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