Anatibant
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.
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- CAS. Nr.: 209733-45-9
- Formel: C34H36Cl2N6O5S
- Molecular Weight:711.66
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Speicherung:
Please store the product under the recommended conditions in the Certificate of Analysis.
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Biologische Aktivität
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Chemical Information
- Reinheit & Dokumentation
- Verweise
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Help & FAQs
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Biologische Aktivität
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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) |
Anatibant binds to the native bradykinin B2 receptor from human umbilical vein (HUV), rat uterus (RU) and guinea-pig ileum (GPI) giving Ki values of 0.89 nM, 0.28 nM and 0.98 nM, respectively[2].
Anatibant inhibits bradykinin-induced IP1, IP2 and IP3 formation in INT407 cells yielding pKB values of 8.5, 8.6 and 8.7, respectively[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Male C57/Bl6 mice (25-28 g) were subjected to Controlled Cortical Impact trauma (CCI)[1]
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Dosage:3 mg/kg
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Administration:Subcutaneous bolus; injection 15 min and 8 h after trauma, respectively
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Result:Demonstrated a significant reduction of ICP and of contusion volume 24 h after trauma in treated mice.
Chemical Information
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CAS. Nr. 209733-45-9
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Molecular Weight 711.66
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Formel C34H36Cl2N6O5S
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SMILES
O=C(NCCCNC(C1=CC=C(C=C1)C(N)=N)=O)[C@H]2N(CCC2)S(=O)(C3=CC=C(C(COC4=C5N=C(C=C(C5=CC=C4)C)C)=C3Cl)Cl)=O
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Synonyms
LF 16-0687; XY-2405
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Versand
Room temperature in continental US; may vary elsewhere.
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Speicherung
Please store the product under the recommended conditions in the Certificate of Analysis.
Reinheit & Dokumentation
Verweise
[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. [Content Brief]
[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. [Content Brief]
Calculators
Konzentration (Stammlösung) × Volumen (Stammlösung) = Konzentration (Ziellösung) × Volumen (Ziellösung)
Anatibant Related Classifications
HY-121156 Related Classifications
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