1. GPCR/G Protein
  2. Bradykinin Receptor
  3. 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.

For research use only. We do not sell to patients.

Anatibant Chemical Structure

Anatibant Chemical Structure

CAS No. : 209733-45-9

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Description

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].

IC50 & Target[2]

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)

In Vitro

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.

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].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

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.
Molecular Weight

711.66

Formula

C34H36Cl2N6O5S

CAS No.
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

Shipping

Room temperature in continental US; may vary elsewhere.

Storage

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

Purity & Documentation
References
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Anatibant Related Classifications

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Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

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Anatibant
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HY-121156
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