| Field | Specification |
|---|---|
| Target | |
| CAS no. | |
| Applications | |
| Molecular weight | |
| Molecular formula | C34H31ClN2O5 |
| Purity | |
| SMILES | |
| Form | Solid |
| Storage | |
| Shipping | |
| Catalog no. (Mfr.) | |
| Main SKU |
Compound Overview
YL-365 selectively antagonizes GPR34, with an IC50 of 17 nM. It occupies part of GPR34's orthosteric binding pocket, triggering allosteric changes that lock the receptor into an inactive state. In M1 microglia, it down-regulates expression of the proinflammatory gene iNOS and dampens proinflammatory responses, and in a mouse model of neuropathic pain it reduces mechanical allodynia in a dose-dependent manner, supporting its use in neuropathic pain research[1]. It is supplied as a white to off-white solid (C34H31ClN2O5, MW 583.07) at 99.96% purity.
Physical & Chemical Properties
| CAS Number | 3077715-58-0 |
|---|---|
| Molecular Formula | C34H31ClN2O5 |
| Molecular Weight | 583.07 g/mol |
| Purity | 99.96% |
| Appearance | Solid |
| Color | White to off-white |
| SMILES | O=C(NC1(C(O)=O)CCN(C(C2=CC=C(C3=CC=CC(Cl)=C3)C=C2)=O)CC1)CC4=CC=C(OCC5=CC=CC=C5)C=C4 |
| Target | GPR34 |
| Signaling Pathway | GPCR/G Protein |
| Solubility | In Vitro: DMSO: 200 mg/mL (343.01 mM; Requires sonication; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO) |
| Storage | 4°C, protect from light. In solvent: -80°C, 6 months; -20°C, 1 month (protect from light). |
| Shipping | Room temperature in continental US; may vary elsewhere. |
Biological Activity
IC50 & Target[1]
|
GPR34 17 nM (IC50) |
Literature Cited
Sources cited in this description and in the In Vitro & In Vivo Data tab. Peer-reviewed publications that used this product are listed under References.
Safety
For Research Use Only. Not for use in diagnostic or therapeutic procedures, and not for human or veterinary use. Handle in accordance with the Safety Data Sheet and your institution's chemical hygiene plan.
In Vitro
| Solvent | Solubility | Notes |
|---|---|---|
| DMSO | 200 mg/mL (343.01 mM) | requires sonication; use freshly opened DMSO (absorbed moisture lowers solubility) |
Aliquot the stock solution and store it at -80°C (up to 6 months) or -20°C (up to 1 month); protect from light; avoid repeated freeze-thaw cycles.
In Vivo
Choose the formulation that suits the animal model and route of administration; percentages are volume ratios of the final working solution. Start from a clear DMSO stock (see In Vitro above), add the co-solvents one at a time in the order listed, mixing after each addition, and prepare the working solution fresh on the day of dosing. If precipitation or phase separation occurs, gentle warming or sonication can help.
Protocol 1
| Composition | 10% DMSO + 90% Corn Oil |
|---|---|
| Result | 5 mg/mL (8.58 mM); clear solution; requires sonication |
| How to prepare | Gives a clear solution at 5 mg/mL. Use with caution if continuous dosing will exceed two weeks. For 1 mL of working solution: add 100 μL DMSO stock (50.0 mg/mL) to 900 μL corn oil. |
Data provided by the manufacturer.
In Vitro
In a cell-based Tango assay, YL-365 potently inhibits GPR34 with an IC50 of 17 nM[1]. Alanine substitutions of key residues in the GPR34 hydrophobic binding pocket significantly reduce the inhibitory potency of YL-365, which confirms the structural binding mode[1]. YL-365 is not cytotoxic to the human cell lines HEK293, LX-2, Beas 2B, and HUVEC (IC50 >100 μM)[1].
In Vivo
In a mouse spinal nerve injury model of neuropathic pain, YL-365 (5-20 mg/kg; i.p.; twice per day) relieves mechanical allodynia in a dose-dependent manner, with significant efficacy at 10 mg/kg and 20 mg/kg, and also lowers iNOS expression in the spinal cord[1]. In mice, YL-365 (200 mg/kg; i.p.; single dose or 100 mg/kg; i.p.; bid; 14 days) is well tolerated[1].
| Animal Model | C57BL/6J mice (neuropathic pain model via L4 spinal nerve transection)[1] |
|---|---|
| Dosage | 5 mg/kg; 10 mg/kg; 20 mg/kg |
| Administration | i.p.; twice per day |
| Result | Increased paw withdrawal threshold. Down-regulated spinal cord proinflammatory gene iNOS expression significantly relative to vehicle controls. Showed no significant effect on spinal cord IL-6, IL-1β, TIMP1, TGF-β, or IL-4 expression. |
Data provided by the manufacturer. Numbered citations refer to the Literature Cited list in the product description.
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