Ki16198

SKU: orb1686573

Description

Ki16198 is an orally bioavailable methyl ester derivative of Ki16425 that acts as a selective LPA1 and LPA3 receptor antagonist, with respective Ki values of 0.34 µM and 0.93 µM. It is utilized in research models, including in vitro signaling assays and in vivo studies investigating pancreatic cancer progression and metastatic spread.

Research Area

Pharmacology & Drug Discovery

Key Properties

• CAS Number: 355025-13-7
• MW: 488.98
• Purity: 97.60% (May vary between batches)
• Formula: C₂₄H₂₅ClN₂O₅S
• SMILES: COC(=O)CCSCc1ccc(cc1)-c1onc(C)c1NC(=O)OC(C)c1ccccc1Cl
• Target: LPL Receptor,LPA Receptor
• Solubility: DMSO:50 mg/mL (102.25 mM);10% DMSO+90% Corn Oil:2.5 mg/mL (5.11 mM);H2O:< 1 mg/mL (insoluble or slightly soluble);Ethanol:33 mg/mL (67.49 mM)

Bioactivity

• Target IC50:
  LPA3:0.93 μM(Ki)|LPA1:0.34 μM(Ki)
• In Vitro:
  Saxagliptin has an inhibition constant Ki of 1.3 nM for DPP4 inhibition, which is 10-fold more potent than either vildagliptin or sitagliptin (another two DPP4 inhibitors) with Ki of 13 and 18 nM. In addition, Saxagliptin demonstrates greater specificity for DPP4 than for either the DPP8 or DPP9 enzymes (400- and 75- fold, respectively). The active metablite of saxagliptin is two-fold less potent than the parent. Both Saxagliptin and its metabolite are highly selective (>4000-fold) for the prevention of DPP4 compared with a range of other proteases (selectivity of sitagliptin and vildagliptin for DPP4 is >2600 and <250-fold, respectively, compared with DPP8 and DPP9). Saxagliptin reduces the degradation of the incretin hormone glucagon-like peptide-1, thereby enhancing its actions, and is associated with improved β-cell function and suppression of glucagon secretion.
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Storage & Handling

• Storage: -20°C
• Expiration Date: 12 months from date of receipt.
• Disclaimer: For research use only

Alternative Names

BxPC-3, Lysophospholipid Receptor, inhibit, Ki16198, Ki 16198, Ki-16198, Inhibitor, lung, liver metastasis, LPL, LPLReceptor, LPL Receptor, LPAReceptor, LPA3, LPA1, LPA Receptor

Compound Identifiers

PubChem CID

9913405