Kuwanon H

SKU: orb1297308

Description

Kuwanon H is a potent non-peptide antagonist selective for the gastrin-releasing peptide (GRP)-preferring bombesin receptor, with a Ki of 290 nM. It is a valuable research tool for investigating the roles of GRP signaling in physiological and pathological contexts, applicable in both in vitro and in vivo experimental models.

Research Area

Metabolism Research, Pharmacology & Drug Discovery

Key Properties

• CAS Number: 76472-87-2
• MW: 760.82
• Purity: 97.99% (May vary between batches)
• Formula: C₄₅H₄₄O₁₁
• SMILES: CC(C)=CCc1c(O)ccc(C(=O)[C@H]2[C@@H](CC(C)=C[C@@H]2c2c(O)cc(O)c3c2oc(c(CC=C(C)C)c3=O)-c2ccc(O)cc2O)c2ccc(O)cc2O)c1O
• Target: Bombesin Receptor,GPCR
• Solubility: 10% DMSO+40% PEG300+5% Tween 80+45% Saline:2 mg/mL (2.63 mM);DMSO:50 mg/mL (65.72 mM)

Bioactivity

• Target IC50:
  GRP:290 nM(Ki)
• In Vitro:
  Kuwanon G and H, isolated from the methanol extract of Morus bombycis, inhibited specific binding of [125I]gastrin-releasing peptide (GRP) to GRP-preferring receptors in murine Swiss 3T3 fibroblasts with Ki values of 470 and 290 nM, respectively. Kuwanon H was one order of magnitude less potent for inhibiting [125I]bombesin binding to neuromedin B (NMB)-preferring receptors in rat esophagus membranes. This compound antagonized bombesin-induced increases in the cytosolic free calcium concentration and GRP-induced DNA synthesis in Swiss 3T3 cells.

Storage & Handling

• Storage: keep away from direct sunlight,keep away from moisture | Powder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice/Shipping at ambient temperature.
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BombesinReceptor, Bombesin Receptor, GPR, inhibit, Inhibitor, Kuwanon H

Compound Identifiers

PubChem CID

5281668