Anatibant
Anatibant Basic information
- Product Name:
- Anatibant
- Synonyms:
-
- anatibant
- (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)-
- Anatibant [inn]
- Unii-clo4jrd21f
- (S)-N-(3-(4-Carbamimidoylbenzamido)propyl)-1-((2,4-dichloro-3-(((2,4-dimethylquinolin-8-yl)oxy)methyl)phenyl)sulfonyl)pyrrolidine-2-carboxamide
- CAS:
- 209733-45-9
- MF:
- C34H36Cl2N6O5S
- MW:
- 711.66
- Mol File:
- 209733-45-9.mol
Anatibant Chemical Properties
- Density
- 1.44±0.1 g/cm3(Predicted)
- pka
- 14.09±0.46(Predicted)
Anatibant Usage And Synthesis
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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Anatibant(209733-45-9)Related Product Information
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- Anatibant
- 4-AMINOMETHYL BENZAMIDINE DIHYDROCHLORIDE
- 4-FORMYL BENZAMIDINE HCL
- 4-AMIDINOBENZAMIDE HYDROCHLORIDE