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.

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Anatibant

Anatibant Estructura química

No. CAS : 209733-45-9

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Descripciòn

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.
Peso molecular

711.66

Fòrmula

C34H36Cl2N6O5S

No. CAS
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

Envío

Room temperature in continental US; may vary elsewhere.

Almacenamiento

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

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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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Inquiry Information

Nombre del producto:
Anatibant
Cat. No.:
HY-121156
Cantidad:
MCE Japan Authorized Agent: