2. GPCR/G Protein Immunology/Inflammation Neuronal Signaling Membrane Transporter/Ion Channel
  3. Mas-related G-protein-coupled Receptor (MRGPR) Interleukin Related Calcium Channel
  4. BER-5

BER-5 is a potent MrgX2 antagonist. BER-5 possess broad-spectrum antagonistic activity against a diverse range of MrgX2 agonists. BER-5 can inhibit Substance P (SP) (HY-P0201)-induced degranulation of LAD2 cells. BER-5 attenuates SP-induced allergic reactions in mice. BER-5 can be used for the study of allergic reactions[1].

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BER-5 Chemical Structure

BER-5 Chemical Structure

CAS No. : 724709-67-5

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BER-5 Related Antibodies

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Description

BER-5 is a potent MrgX2 antagonist. BER-5 possess broad-spectrum antagonistic activity against a diverse range of MrgX2 agonists. BER-5 can inhibit Substance P (SP) (HY-P0201)-induced degranulation of LAD2 cells. BER-5 attenuates SP-induced allergic reactions in mice. BER-5 can be used for the study of allergic reactions[1].

In Vitro

BER-5 (12.5-50 μM) inhibits SP-induced degranulation of LAD2 cells specifically manifested by the suppression of β-hexosaminidase (30 min), histamine (2 h), and IL-8 release (6 h)[1].

BER-5 (0-100 μM ,30 min) (IC50 = 20.64 μM) inhibit the SP-induced release of β-hexosaminidase more effectively in LAD2 cells compared with Bergaptol (BER; HY-76316) (IC50 = 46.79 μM) and Imperatorin (IMP; HY-N0285) (IC50 = 99.73 μM)[1].

BER-5 (50 μM) slightly increased the half-maximal effective concentration (EC50) while significantly decreasing the maximum efficiency (Emax) response of SP in LAD2 cells[1].

BER-5 (12.5-50 μM) inhibits degranulation induced by C48/80 (HY-130592), (R)-ZINC-3573 (HY-118069), Rocuronium Bromide (HY-17440) and Ciprofloxacin (HY-B0356) in LAD2 cells, suggesting that BER-5 possess broad-spectrum antagonistic activity against a diverse range of MrgX2 agonists[1].

BER-5 (12.5-50 μM, 30 min) inhibits Ca2+ mobilization induced by SP in a concentration-dependent manner in MrgX2-HEK293 cells[1].

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

BER-5 Related Antibodies
In Vivo

BER-5 (6.25-25 mg/kg, i.g., single dose) attenuates SP-Induced Allergic Reactions in the adult mice[1].

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

Animal Model: 6-8 weeks adult male C57BL/6 mice treated SP (10 μM)
Dosage: 6.25, 12.5, 25 mg/kg
Administration: i.g. 2 h before anesthetize
Result: Attenuated SP-induced local paw swelling and Evans blue exudation dose-dependently.
Mitigated SP-induced vasodilation and inhibited mast cell deformation and degranulation.
Reduced plasma histamine concentrations in a dose-dependent manner.
Molecular Weight

320.34

Formula

C20H16O4
CAS No.
SMILES

O=C1C=CC2=C(C3=C(OC=C3)C=C2O1)OCCCC4=CC=CC=C4
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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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BER-5 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.

Keywords:

BER-5724709-67-5BER5BER 5Mas-related G-protein-coupled Receptor (MRGPR)Interleukin RelatedCalcium ChannelILCa2+ channelsCa channelsMrgX2GPCRsLAD2allergic reactionssubstance PInhibitorinhibitorinhibit

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