YL-365
Based on 1 Customer Validation
YL-365 is a potent and selective GPR34 antagonist with an IC50 of 17 nM. YL-365 binds to a portion of the orthosteric binding pocket of GPR34 and induces allosteric changes that stabilize the receptor in an inactive conformation. YL-365 down-regulates expression of the proinflammatory gene iNOS in M1 microglia and suppresses proinflammatory responses. YL-365 reduces mechanical allodynia in a dose-dependent manner in a mouse model of neuropathic pain. YL-365 can be used for the research of neuropathic pain.
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- Purity: 99.96%
- CAS No.: 3077715-58-0
- 화학식: C34H31ClN2O5
- 분자량:583.07
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보관:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
To place orders, for customer services and technical support, please contact: MedChemExpress USA
Tel: 609-228-6898 E-mail: [email protected] [email protected]
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Help & FAQs
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Biological Activity
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GPR34 17 nM (IC50) |
YL-365 potently inhibits GPR34 in a cell-based Tango assay with an IC50 of 17 nM[1].
YL-365 has its inhibitory potency significantly reduced by alanine substitutions of key residues in the GPR34 hydrophobic binding pocket, confirming the structural binding mode[1].
YL-365 shows no cytotoxicity against human HEK293, LX-2, Beas 2B, and HUVEC cell lines (IC50 >100 μM)[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
| Species | Dose | Route | AUC0-∞ | T1/2 | CL |
|---|---|---|---|---|---|
| Mice[1] | 20 mg/kg | i.p. | 6614.77 ng·h/mL | 1.315 h | 50.15 mL/min/kg |
YL-365 (200 mg/kg; i.p.; single dose or 100 mg/kg; i.p.; bid; 14 days) shows good safety in mice[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:C57BL/6J mice (neuropathic pain model via L4 spinal nerve transection)[1]
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Dosage:5 mg/kg; 10 mg/kg; 20 mg/kg
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Administration:i.p.; twice per day
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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.
Chemical Information
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CAS No. 3077715-58-0
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Appearance Solid
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분자량 583.07
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화학식 C34H31ClN2O5
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Color White to off-white
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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
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
용액&용해도
DMSO : 200 mg/mL (343.01 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
Select the appropriate dissolution method based on your experimental animal and administration route.
- For the following dissolution methods, please ensure to first prepare a clear stock solution using an In Vitro approach and then sequentially add co-solvents:
- To ensure reliable experimental results, the clarified stock solution can be appropriately stored based on storage conditions. As for the working solution for In Vivo experiments, it is recommended to prepare freshly and use it on the same day.
- The percentages shown for the solvents indicate their volumetric ratio in the final prepared solution. If precipitation or phase separation occurs during preparation, heat and/or sonication can be used to aid dissolution.
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.
Please enter your animal formula composition:
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%DMSO +
Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
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%+
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+%Tween-80 + +
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%Saline +
The co-solvents required include: DMSO, . All of co-solvents are available by MedChemExpress (MCE). , Tween 80. All of co-solvents are available by MedChemExpress (MCE).
Working solution concentration: 0.22 mg/mL
Method for preparing stock solution: mg drug dissolved in μL DMSO. Stock solution concentration: mg/mL. * In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
1. Take μL DMSO stock solution;
2. Add μL .
μL , mix evenly;
3. Then add μL Tween 80, mix evenly;
4. Then add μL
Please ensure that the stock solution in the first step is dissolved to a clear state, and add co-solvents in sequence. You can use ultrasonic heating (ultrasonic cleaner, recommended frequency 20-40 kHz), vortexing, etc. to assist dissolution.
순도&문서
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Data Sheet (271 KB)
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SDS (251 KB)
- English - EN (251 KB)
- Français - FR (251 KB)
- Deutsch - DE (251 KB)
- Norwegian - NO (251 KB)
- Español - ES (251 KB)
- Swedish - SV (251 KB)
- Italian - IT (251 KB)
- Korean - KR (251 KB)
- Portuguese - PT (251 KB)
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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 (protect from light). 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 | 1.7151 mL | 8.5753 mL | 17.1506 mL | 42.8765 mL |
| 5 mM | 0.3430 mL | 1.7151 mL | 3.4301 mL | 8.5753 mL | |
| 10 mM | 0.1715 mL | 0.8575 mL | 1.7151 mL | 4.2876 mL | |
| 15 mM | 0.1143 mL | 0.5717 mL | 1.1434 mL | 2.8584 mL | |
| 20 mM | 0.0858 mL | 0.4288 mL | 0.8575 mL | 2.1438 mL | |
| 25 mM | 0.0686 mL | 0.3430 mL | 0.6860 mL | 1.7151 mL | |
| 30 mM | 0.0572 mL | 0.2858 mL | 0.5717 mL | 1.4292 mL | |
| 40 mM | 0.0429 mL | 0.2144 mL | 0.4288 mL | 1.0719 mL | |
| 50 mM | 0.0343 mL | 0.1715 mL | 0.3430 mL | 0.8575 mL | |
| 60 mM | 0.0286 mL | 0.1429 mL | 0.2858 mL | 0.7146 mL | |
| 80 mM | 0.0214 mL | 0.1072 mL | 0.2144 mL | 0.5360 mL | |
| 100 mM | 0.0172 mL | 0.0858 mL | 0.1715 mL | 0.4288 mL |
YL-365 Related Classifications
HY-156815 Related Classifications
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