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^[1][2][3].

The D-enantiomer of NAPAP is a highly selective, potent direct thrombin inhibitor with a K_i 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 (1 mg/kg; intravenous administration; single bolus injection) is rapidly systemically cleared in female Wistar rats, with extensive hepatobiliary excretion as its primary elimination pathway^[1].
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.

521.63

C₂₇H₃₁N₅O₄S

137171-40-5

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

Room temperature in continental US; may vary elsewhere.

Please store the product under the recommended conditions in the Certificate of Analysis.

• [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]