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.
商品は「研究用試薬」です。人や動物の医療用・臨床診断用・食品用の製品ではありません。
研究用途以外に使用した場合、当社は一切の責任を負いかねます。
- CAS 番号: 209733-45-9
- 分子式: C34H36Cl2N6O5S
- 分子量:711.66
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保管条件:
Please store the product under the recommended conditions in the Certificate of Analysis.
Bradykinin Receptor アイソフォーム固有の製品をすべて表示
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生物活性
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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.
化学情報
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CAS 番号 209733-45-9
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分子量 711.66
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分子式 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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別名
LF 16-0687; XY-2405
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輸送条件
Room temperature in continental US; may vary elsewhere.
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保管条件
Please store the product under the recommended conditions in the Certificate of Analysis.
純度とドキュメンテーション
参考文献
[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
濃度 (開始) × 体積 (開始) = 濃度 (終了) × 体積 (終了)