1. GPCR/G Protein
  2. LPL Receptor

Ki16425 

Cat. No.: HY-13285 Purity: 98.67%
Handling Instructions

Ki16425 is a competitive, potent and reversible antagonist to LPA1, LPA2 and LPA3 with Ki of 0.34 μM, 6.5 μM and 0.93 μM, respectively, shows no activity at LPA4, LPA5, LPA6.

For research use only. We do not sell to patients.

Ki16425 Chemical Structure

Ki16425 Chemical Structure

CAS No. : 355025-24-0

Size Price Stock Quantity
10 mM * 1 mL in DMSO USD 66 In-stock
Estimated Time of Arrival: December 31
5 mg USD 60 In-stock
Estimated Time of Arrival: December 31
10 mg USD 108 In-stock
Estimated Time of Arrival: December 31
50 mg USD 432 In-stock
Estimated Time of Arrival: December 31
100 mg   Get quote  
200 mg   Get quote  

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  • Biological Activity

  • Technical Information

  • Purity & Documentation

  • References

Description

Ki16425 is a competitive, potent and reversible antagonist to LPA1, LPA2 and LPA3 with Ki of 0.34 μM, 6.5 μM and 0.93 μM, respectively, shows no activity at LPA4, LPA5, LPA6. IC50 value: 0.3/6.5/0.93 uM(Ki, LPA1/2/3) [1] Target: LPA1/2/3 in vitro: Kil6425 preferentially inhibits LPA1- and LPA3-mediated responses but has only a moderate effect on LPA2. Ki16425 inhibits the LPA-induced Ca(2+) response in THP-1 cells, 3T3 fibroblasts, and A431 cells, but had only a marginal effect in PC-12 cells and HL-60 cells, which means that Ki16425 seems to be a useful tool for evaluating the involvement of specific LPA receptors in the short-term response to LPA. Ki16425 inhibits long-term DNA synthesis and cell migration as induced by LPA in Swiss 3T3 fibroblasts [1]. Ki16425 reduces the LPA-induced activation of p42/p44 mitogen activated protein kinase (MAPK), while acting as a weak stimulator of p42/p44 MAPK on its own, properties typical of a protean agonist. Ki16425 also significantly reduces the NGF-induced stimulation of p42/p44 MAPK and inhibited NGF-stimulated neurite outgrowth in PC-12 cells [2]. in vivo: Ki-16425 (30 mg/kg, i.p.) completely blocks LPA-induced neuropathic pain-like behaviors, when administered 30 min but not 90 min before lysophosphatidic acid injection, suggesting that Ki-16425 is a short-lived inhibitor. Ki-16425 also inhibits nerve injury-induced up-regulation of Caα2δ-1 in the dorsal root ganglion and reduction of SP immunoreactivity in the spinal dorsal horn [3].

Solvent & Solubility
In Vitro: 

10 mM in DMSO

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.1054 mL 10.5272 mL 21.0544 mL
5 mM 0.4211 mL 2.1054 mL 4.2109 mL
10 mM 0.2105 mL 1.0527 mL 2.1054 mL
*Please refer to the solubility information to select the appropriate solvent.
References
Molecular Weight

474.96

Formula

C₂₃H₂₃ClN₂O₅S

CAS No.

355025-24-0

SMILES

ClC1=C(C=CC=C1)C(C)OC(NC2=C(ON=C2C)C3=CC=C(C=C3)CSCCC(O)=O)=O

Storage
Powder -20°C 3 years
  4°C 2 years
In solvent -80°C 6 months
  -20°C 1 month
Shipping

Room temperature in continental US; may vary elsewhere

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Product Name:
Ki16425
Cat. No.:
HY-13285
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Ki16425

Cat. No.: HY-13285