| Identification | Back Directory | [Name]
Anatibant | [CAS]
209733-45-9 | [Synonyms]
anatibant
Anatibant [inn]
Unii-clo4jrd21f
(2s)-n-(3-(4-carbamimidoylbenzamido)propyl)-1-(2,4-dichloro-3-((2,4-dimethyl-8-quinolyloxy)methyl)phenylsulfonyl)pyrrolidine-2-carboxamide
2-PYRROLIDINECARBOXAMIDE, N-[3-[[4-(AMINOIMINOMETHYL)BENZOYL]AMINO]PROPYL]-1-[[2,4-DICHLORO-3-[[(2,4-DIMETHYL-8-QUINOLINYL)OXY]METHYL]PHENYL]SULFONYL]-, (2S)- | [Molecular Formula]
C34H36Cl2N6O5S | [MDL Number]
MFCD09833920 | [MOL File]
209733-45-9.mol | [Molecular Weight]
711.658 |
| Hazard Information | Back Directory | [Uses]
Anatibant (LF 16-0687; XY-2405) is a selective non-peptide bradykinin B2 receptor antagonist. Anatibant binds to the human, rat and guinea-pig recombinant B2 receptor with Ki values of 0.67 nM, 1.74 nM and 1.37 nM, respectively. Anatibant crosses the blood-brain barrier (BBB). Anatibant can be used in research on brain damage diseases[1][2]. | [Definition]
ChEBI: Anatibant is a proline derivative. | [in vivo]
Anatibant (3 mg/kg; subcutaneous bolus; injection 15 min and 8 h after trauma, respectively) significantly reduces intracranial pressure (ICP) and of contusion volume 24 h after trauma in treated mice[1]. | Animal Model: | Male C57/Bl6 mice (25-28 g) were subjected to Controlled Cortical Impact trauma (CCI)[1] | | Dosage: |
3 mg/kg | | Administration: | Subcutaneous bolus; injection 15 min and 8 h after trauma, respectively | | Result: | Demonstrated a significant reduction of ICP and of contusion volume 24 h after trauma in treated mice. |
| [IC 50]
Bradykinin B2 Receptor (B2R): 0.67 nM (Ki, human recombinant B2 receptor); Bradykinin B2 Receptor (B2R): 1.74 nM (Ki, Rat recombinant B2 receptor); Bradykinin B2 Receptor (B2R): 1.37 nM (Ki, Guinea-pig recombinant B2 receptor) | [References]
[1] Klaus Zweckberger, et al. Anatibant, a selective non-peptide bradykinin B2 receptor antagonist, reduces intracranial hypertension and histopathological damage after experimental traumatic brain injury. Neurosci Lett. 2009 Apr 24;454(2):115-7. DOI:10.1016/j.neulet.2009.02.014
[2] D Pruneau, et al. Pharmacological profile of LF 16-0687, a new potent non-peptide bradykinin B2 receptor antagonist. Immunopharmacology. 1999 Sep;43(2-3):187-94. DOI:10.1016/s0162-3109(99)00128-9 |
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LGM Pharma
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Alfa Chemistry
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www.alfa-chemistry.com |
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Wonda Science
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