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Ki16198

Catalog No. T6347 CAS 355025-13-7

Ki16198 is the methyl ester of Ki16425, which is a LPA antagonist and inhibits LPA1- and LPA3-induced inositol phosphate production with Ki of 0.34 μM and 0.93 μM, respectively, shows weaker inhibition for LPA2, no activity at LPA4, LPA5, LPA6.

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Ki16198, CAS 355025-13-7

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Purity: 98%

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Description	Ki16198 is the methyl ester of Ki16425, which is a LPA antagonist and inhibits LPA1- and LPA3-induced inositol phosphate production with Ki of 0.34 μM and 0.93 μM, respectively, shows weaker inhibition for LPA2, no activity at LPA4, LPA5, LPA6.
Targets&IC50	LPA1:0.34 μM(Ki), LPA3:0.93 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). [2] 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. [3]

Molecular Weight	488.98
Formula	C24H25ClN2O5S
CAS No.	355025-13-7

Storage

Powder: -20°C for 3 years

In solvent: -80°C for 2 years

Solubility Information

DMSO: 89 mg/mL (182 mM)

Ethanol: 33 mg/mL (67.5 mM)

H2O: <1 mg/mL

( < 1 mg/ml refers to the product slightly soluble or insoluble )

References and Literature

1. Komachi M, et al. Cancer Sci, 2012, 103(6), 1099-1104. 2. Shano S, et al. Biochim Biophys Acta, 2008, 1783(5), 748-759.

Related Products

Related compounds with same targets

TAK-615 Tetradecyl Phosphonate ONO-7300243 Ki16198 TC LPA5 4 H2L5186303 GRI977143 DBIBB

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Keywords

Ki16198 355025-13-7 G蛋白偶联受体 LPA Receptor LPL Receptor lung Ki 16198 inhibit Inhibitor BxPC-3 liver metastasis Ki-16198 Lysophospholipid Receptor inhibitor

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