2. GPCR/G Protein Apoptosis
  3. LPL Receptor Apoptosis
  4. H2L5186303

H2L5186303 is an effective and selective LPA2 receptor antagonist, with an IC50 of 9 nM, and it has anti-inflammatory effects. H2L5186303 can inhibit intestinal cell proliferation and promote apoptosis.

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

H2L5186303 Chemical Structure

H2L5186303 Chemical Structure

CAS No. : 139262-76-3

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Solid + Solvent (Highly Recommended)
10 mM * 1 mL in DMSO
ready for reconstitution
 USD 143 In-stock
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10 mM * 1 mL in DMSO USD 143 In-stock
Solid
5 mg USD 130 In-stock
10 mg USD 220 In-stock
25 mg USD 480 In-stock
50 mg USD 820 In-stock
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Customer Review

Based on 1 publication(s) in Google Scholar

H2L5186303 Related Antibodies

Top Publications Citing Use of Products

1 Publications Citing Use of MCE H2L5186303

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LPAR1 LPAR2 LPAR3 LPAR5 S1PR1 S1PR2 S1PR3 S1PR4 S1PR5

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Description

H2L5186303 is an effective and selective LPA2 receptor antagonist, with an IC50 of 9 nM, and it has anti-inflammatory effects. H2L5186303 can inhibit intestinal cell proliferation and promote apoptosis[1][2][3].

IC50 & Target

LPA2 Receptor

9 nM (IC50)

In Vitro

H2L5186303 (0.3-10 μM, 30 min) inhibits mast cell degranulation[2].
H2L5186303 (10 μM, 2 days) inhibits LPA2 and promotes apoptosis in intestinal epithelial cells (IEC)[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

H2L5186303 Related Antibodies

Apoptosis Analysis[3]

Cell Line: IECs
Concentration: 10 μM
Incubation Time: 0 and 2 days
Result: Blocked intestinal-like growth, reduced cell proliferation, and increased cell apoptosis.
In Vivo

H2L5186303 (0-50 mg/kg, given by intraperitoneal injection, single dose) suppresses the levels of eosinophils and lymphocytes in OVA-sensitized mice, and has the trachea inflammation inhibitory effect[2].
H2L5186303 (10 mg/kg, given by intraperitoneal injection, three times every other day, 6 days) inhibits cell proliferation in Lpar5f/f Villin-Cre mice intestinal crypts and promotes apoptosis[3].

MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.

Animal Model: Ovalbumin-Induced allergic asthma in BALB/c mice[2]
Dosage: 1 mg/kg, single dose; 0, 6.25, 12.5, 25, 50 mg/mL, single dose
Administration: Intraperitoneal injection (i.p.)
Result: Showed strong inhibitory effects, reducing airway hyper-responsiveness, levels of inflammatory cytokines, mucus production, and the number of eosinophils before sensitization and toxin exposure in OVA.
Lowered AHR and inflammation scores.
Suppressed mRNA levels of IL-4, IL-13, and IFN-γ, but did not inhibit IgE levels.
Animal Model: Lpar5f/f Villin-Cre mice[3]
Dosage: 10 mg/kg, every other day for three times, 6 days
Administration: Intraperitoneal injection (i.p.)
Result: Reduced the number of proliferating cells in the intestinal crypts of mice and increased cell apoptosis.
Molecular Weight

488.45

Formula

C26H20N2O8
CAS No.
Appearance

Solid

Color

Light yellow to yellow

SMILES

OC(/C=C\C(NC(C=C1)=CC=C1OC2=CC=CC(OC3=CC=C(C=C3)NC(/C=C\C(O)=O)=O)=C2)=O)=O
Shipping

Room temperature in continental US; may vary elsewhere.
Storage
Powder -20°C 3 years
4°C 2 years
In solvent -80°C 6 months
-20°C 1 month
Solvent & Solubility
In Vitro: 

DMSO : 250 mg/mL (511.82 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)

Preparing
Stock Solutions
Concentration Solvent Mass 1 mg 5 mg 10 mg
1 mM 2.0473 mL 10.2365 mL 20.4729 mL
5 mM 0.4095 mL 2.0473 mL 4.0946 mL
View the Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

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This equation is commonly abbreviated as: C1V1 = C2V2

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In Vivo Dissolution Calculator
Please enter the basic information of animal experiments:

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Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.
Calculation results:
Working solution concentration: mg/mL
Purity & Documentation

Purity: 98.72%

SDS (251 KB)

COA (243 KB) HNMR (288 KB) LCMS (266 KB)

Handling Instructions (2659 KB)
References

Complete Stock Solution Preparation Table

* Please refer to the solubility information to select the appropriate solvent. Once prepared, please aliquot and store the solution to prevent product inactivation from repeated freeze-thaw cycles.
Storage method and period of stock solution: -80°C, 6 months; -20°C, 1 month. When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.

Optional Solvent Concentration Solvent Mass 1 mg 5 mg 10 mg 25 mg
DMSO 1 mM 2.0473 mL 10.2365 mL 20.4729 mL 51.1823 mL
5 mM 0.4095 mL 2.0473 mL 4.0946 mL 10.2365 mL
10 mM 0.2047 mL 1.0236 mL 2.0473 mL 5.1182 mL
15 mM 0.1365 mL 0.6824 mL 1.3649 mL 3.4122 mL
20 mM 0.1024 mL 0.5118 mL 1.0236 mL 2.5591 mL
25 mM 0.0819 mL 0.4095 mL 0.8189 mL 2.0473 mL
30 mM 0.0682 mL 0.3412 mL 0.6824 mL 1.7061 mL
40 mM 0.0512 mL 0.2559 mL 0.5118 mL 1.2796 mL
50 mM 0.0409 mL 0.2047 mL 0.4095 mL 1.0236 mL
60 mM 0.0341 mL 0.1706 mL 0.3412 mL 0.8530 mL
80 mM 0.0256 mL 0.1280 mL 0.2559 mL 0.6398 mL
100 mM 0.0205 mL 0.1024 mL 0.2047 mL 0.5118 mL
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H2L5186303 Related Classifications

Help & FAQs
  • Do most proteins show cross-species activity?

    Species cross-reactivity must be investigated individually for each product. Many human cytokines will produce a nice response in mouse cell lines, and many mouse proteins will show activity on human cells. Other proteins may have a lower specific activity when used in the opposite species.

Keywords:

H2L5186303139262-76-3LPL ReceptorApoptosisLysophospholipid ReceptorAnti-inflammatoryIntestinal cellsCell apoptosisInhibitorinhibitorinhibit

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