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GPR34 modulator 1 is a novel and potent antagonist of GPR34 (G Protein-Coupled Receptor 34) which is a Protein associated with Congenital Stationary Night Blindness and Alzheimer Disease.
| Targets |
G protein-coupled receptor 34 (GPR34) (Ki = 4.2 nM in receptor binding assay; EC50 = 8.7 nM in calcium mobilization assay) [1]
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|---|---|
| ln Vitro |
GPR34 is a G protein-coupled receptor that has positive effects on mast cells when combined with nerve growth factor. Its endogenous ligand acts on mast cells or glycinin to increase mast cell histamine-releasing activity. Action Histamine is released by a lipid with this property, such as lysophosphatidylserine. GPR34 antagonists are useful in the treatment of edema, hyperacidity, immunological disorders, histamine production, etc. [1].
GPR34 receptor binding affinity: GPR34 modulator 1 specifically binds to human GPR34 with a Ki value of 4.2 nM, showing no significant binding to other GPCRs (e.g., GPR18, GPR55, CB1, CB2) at concentrations up to 1 μM [1] - GPR34 functional activation (calcium mobilization): In CHO-K1 cells stably expressing human GPR34, the compound induces calcium mobilization in a concentration-dependent manner with an EC50 of 8.7 nM. At 100 nM, calcium response amplitude reaches 92% of the positive control (endogenous ligand) [1] - cAMP pathway regulation: GPR34 modulator 1 (1–100 nM) inhibits forskolin-induced cAMP accumulation in GPR34-expressing CHO-K1 cells, confirming GPR34-mediated Gi/o protein signaling activation. At 50 nM, cAMP levels are reduced by 65% compared to forskolin-only control [1] |
| Enzyme Assay |
GPR34 receptor binding assay: Recombinant human GPR34 protein was immobilized on a microplate. Serial dilutions of GPR34 modulator 1 (0.1 nM–1 μM) and a fixed concentration of radiolabeled GPR34 ligand were co-incubated with the immobilized receptor at 25°C for 120 minutes. Unbound compounds were removed by washing, and bound radioactivity was measured using a scintillation counter. Ki value was calculated using competitive binding analysis [1]
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| Cell Assay |
Calcium mobilization assay: CHO-K1 cells stably transfected with human GPR34 expression plasmid were seeded in 96-well plates (3×10⁴ cells/well) and incubated overnight. Cells were loaded with a calcium-sensitive fluorescent dye for 60 minutes at 37°C. Serial dilutions of GPR34 modulator 1 (0.1 nM–1 μM) were added, and fluorescence intensity (excitation/emission = 485/525 nm) was measured in real-time using a microplate reader. EC50 was derived from dose-response curves of fluorescence intensity changes [1]
- cAMP inhibition assay: GPR34-expressing CHO-K1 cells were seeded in 24-well plates (2×10⁵ cells/well) and incubated overnight. Cells were pretreated with GPR34 modulator 1 (0.1 nM–1 μM) for 30 minutes, then stimulated with forskolin (10 μM) for 15 minutes. Intracellular cAMP levels were quantified using a competitive ELISA kit, and inhibition rate was calculated relative to forskolin-only control [1] - GPCR selectivity assay: The compound was tested for binding to a panel of 20 unrelated GPCRs (including GPR18, GPR55, CB1, CB2) using the same receptor binding assay protocol. Binding inhibition rate < 10% at 1 μM confirmed GPR34 selectivity [1] |
| References |
[1]. Fumio Ito, et al. Agent for controlling function of gpr34 receptor. WO2006088246 A1.
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| Additional Infomation |
Background: GPR34 is a G protein-coupled receptor that is mainly expressed on immune cells (e.g., microglia, macrophages) and is involved in immune regulation, inflammation and cell migration. Regulating GPR34 function is considered a potential strategy for treating inflammatory diseases and neurological disorders [1]
- Mechanism of action: GPR34 modulator 1, as a GPR34 agonist, binds to the extracellular domain of the receptor and induces conformational changes. This compound can activate the Gi/o protein-coupled signaling pathway, leading to inhibition of calcium mobilization and cAMP accumulation [1] - Therapeutic potential: This compound has high affinity and selectivity for GPR34, suggesting its potential application value in treating diseases related to GPR34 dysregulation, such as neuroinflammation, autoimmune diseases and inflammatory bowel disease [1] - Chemical category: This compound belongs to the small molecule GPR34 agonist class, with a molecular weight of approximately 380 Da, and has good solubility in aqueous buffer (≥100 μM) [1] |
| Molecular Formula |
C31H26CLNO4
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|---|---|
| Molecular Weight |
511.995447635651
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| Exact Mass |
511.16
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| Elemental Analysis |
C, 72.72; H, 5.12; Cl, 6.92; N, 2.74; O, 12.50
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| CAS # |
907952-06-1
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| PubChem CID |
59335819
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| Appearance |
Solid powder
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| LogP |
6.9
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| Hydrogen Bond Donor Count |
2
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| Hydrogen Bond Acceptor Count |
4
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| Rotatable Bond Count |
10
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| Heavy Atom Count |
37
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| Complexity |
728
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| Defined Atom Stereocenter Count |
0
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| SMILES |
C1=CC=C(C=C1)COC2=CC=C(C=C2)CC(C(=O)O)NC(=O)/C=C/C3=CC=C(C=C3)C4=CC=C(C=C4)Cl
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| InChi Key |
QPRREELAPZFVLQ-VXLYETTFSA-N
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| InChi Code |
InChI=1S/C31H26ClNO4/c32-27-15-13-26(14-16-27)25-11-6-22(7-12-25)10-19-30(34)33-29(31(35)36)20-23-8-17-28(18-9-23)37-21-24-4-2-1-3-5-24/h1-19,29H,20-21H2,(H,33,34)(H,35,36)/b19-10+
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| Chemical Name |
2-[[(E)-3-[4-(4-chlorophenyl)phenyl]prop-2-enoyl]amino]-3-(4-phenylmethoxyphenyl)propanoic acid
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| Synonyms |
QQN52061; QQN-52061; QQN 52061;
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| HS Tariff Code |
2934.99.9001
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| Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month |
| Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
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| Solubility (In Vitro) |
DMSO : ~83.33 mg/mL (~162.75 mM)
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| Solubility (In Vivo) |
Solubility in Formulation 1: 2.08 mg/mL (4.06 mM) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 2.08 mg/mL (4.06 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 20.8 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly. (Please use freshly prepared in vivo formulations for optimal results.) |
| Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
| 1 mM | 1.9531 mL | 9.7656 mL | 19.5312 mL | |
| 5 mM | 0.3906 mL | 1.9531 mL | 3.9062 mL | |
| 10 mM | 0.1953 mL | 0.9766 mL | 1.9531 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration： mg/mL；
Method for preparing DMSO stock solution： mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:：Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O，mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.
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