NAPAP
NAPAP is a selective direct thrombin inhibitor. NAPAP rapidly binds to thrombin and inhibits its activity, and reduces LPS (HY-D1056)-induced brain inflammation and coagulation factor expression in vivo. NAPAP can be used in studies related to coagulation and neuroinflammation.
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- CAS No.: 137171-40-5
- Formule: C27H31N5O4S
- Masse moléculaire:521.63
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Stockage:
Please store the product under the recommended conditions in the Certificate of Analysis.
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Activité biologique
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Chemical Information
- Pureté et documentation
- Références
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Help & FAQs
Activité biologique
The D-enantiomer of NAPAP is a highly selective, potent direct thrombin inhibitor with a Ki of 0.0021 μM for thrombin, fast binding kinetics, and weak activity against trypsin, factor Xa, and plasmin[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
NAPAP (0.75 mg/kg; intraperitoneal injection; single administration) significantly reduces the hippocampal expression of pro-inflammatory markers and coagulation factors induced by LPS (HY-D1056) in male C57BL/6 mice[2].
NAPAP (400-1300 mg/kg; intraperitoneal injection; single administration) induces dose-dependent mortality, hepatotoxicity, and hepatic covalent binding in male ddY mice, with an LD50 of 820 mg/kg in control animals, while LPS pretreatment attenuates these toxic effects in a dose-dependent manner[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6 (8-week-old, male)[2]
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Dosage:0.75 mg/kg
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Administration:i.p.; single concurrent dose with LPS injection
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Result:Reduced hippocampal gene expression of TNFα, CXL9, CCL1.
Reduced hippocampal gene expression of coagulation factor FX, PAR1.
Chemical Information
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CAS No. 137171-40-5
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Masse moléculaire 521.63
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Formule C27H31N5O4S
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SMILES
N=C(N)C(C=C1)=CC=C1C[C@H](C(N2CCCCC2)=O)NC(CNS(=O)(C3=CC4=C(C=CC=C4)C=C3)=O)=O
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Please store the product under the recommended conditions in the Certificate of Analysis.
Pureté et documentation
Références
[1]. Steinmetzer T, et al. Structure-activity relationships of new NAPAP-analogs. J Enzyme Inhib Med Chem. 2002;17(2):241-249. [Content Brief]
[2]. Shavit Stein E, et al. Thrombin Inhibition Reduces the Expression of Brain Inflammation Markers upon Systemic LPS Treatment. Neural Plast. 2018;2018:7692182. Published 2018 Jun 19. [Content Brief]
[3]. Ishikawa M, et al. Antidotal effect of lipopolysaccharide against acetaminophen-induced mortality in mice. Pharmacol Toxicol. 1990;67(5):387-391. [Content Brief]
Calculators
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
NAPAP Related Classifications
HY-174285 Related Classifications
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