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Ki16198

Ki16198
Ki16198 is an orally available LPA receptor antagonist and is a methyl ester derivative of Ki16425. It inhibits LPA1- and LPA3-induced inositol phosphates with Ki values of 0.34 and 0.93 μM, respectively, and can be used in studies of pancreatic carcinogenesis and metastasis.
Catalog No. T6347Cas No. 355025-13-7
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Purity:97.6%
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Ki16198

Catalog No. T6347Cas No. 355025-13-7
Ki16198 is an orally available LPA receptor antagonist and is a methyl ester derivative of Ki16425. It inhibits LPA1- and LPA3-induced inositol phosphates with Ki values of 0.34 and 0.93 μM, respectively, and can be used in studies of pancreatic carcinogenesis and metastasis.
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Pack SizePriceAvailabilityQuantity
5 mg$48In Stock
10 mg$83In Stock
25 mg$173In Stock
50 mg$273In Stock
100 mg$395In Stock
500 mg$858In Stock
1 mL x 10 mM (in DMSO)$53In Stock
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Product Introduction

Bioactivity
Description
Ki16198 is an orally available LPA receptor antagonist and is a methyl ester derivative of Ki16425. It inhibits LPA1- and LPA3-induced inositol phosphates with Ki values of 0.34 and 0.93 μM, respectively, and can be used in studies of pancreatic carcinogenesis and metastasis.
Targets&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). [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]
Chemical Properties
Molecular Weight488.98
FormulaC24H25ClN2O5S
Cas No.355025-13-7
Storage & Solubility Information
StoragePowder: -20°C for 3 years | In solvent: -80°C for 1 year | Shipping with blue ice.
Solubility Information
DMSO: 50 mg/mL (102.25 mM)
Ethanol: 33 mg/mL (67.5 mM)
H2O: < 1 mg/mL (insoluble or slightly soluble)
Solution Preparation Table
Ethanol/DMSO
1mg5mg10mg50mg
1 mM2.0451 mL10.2254 mL20.4507 mL102.2537 mL
5 mM0.4090 mL2.0451 mL4.0901 mL20.4507 mL
10 mM0.2045 mL1.0225 mL2.0451 mL10.2254 mL
20 mM0.1023 mL0.5113 mL1.0225 mL5.1127 mL
50 mM0.0409 mL0.2045 mL0.4090 mL2.0451 mL
DMSO
1mg5mg10mg50mg
100 mM0.0205 mL0.1023 mL0.2045 mL1.0225 mL

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