Art. -Nr.: HY-156815

YL-365

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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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Reinheit: 99.96%
CAS. Nr.: 3077715-58-0
Formel: C₃₄H₃₁ClN₂O₅
Molecular Weight:583.07

Speicherung:

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

YL-365 Chemical Structure

CAS. Nr.: 3077715-58-0

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Preis

Verfügbarkeit

Menge

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Strong Fluorescence Signal / Multi-Disciplinary Applications / High Fluorescence Specificity

Biologische Aktivität
- Beschreibung
- IC₅₀ & Target
- In Vitro
- Parmacokinetics
- In Vivo
Chemical Information
Lösungsmittel & Löslichkeit
- In Vitro
- In Vivo
Reinheit & Dokumentation
Verweise
Help & FAQs
Classifications
Bioz

Biologische Aktivität

Beschreibung

IC₅₀ & Target^[1]

GPR34

17 nM (IC₅₀)

In Vitro

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.

Parmacokinetics

Species	Dose	Route	AUC_0-∞	T_1/2	CL
Mice^[1]	20 mg/kg	i.p.	6614.77 ng·h/mL	1.315 h	50.15 mL/min/kg

In Vivo

YL-365 (5-20 mg/kg; i.p.; twice per day) dose-dependently alleviates mechanical allodynia in a mouse spinal nerve injury model of neuropathic pain, with significant efficacy observed at 10 mg/kg and 20 mg/kg, and reduces spinal cord iNOS expression^[1].
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.

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.

Chemical Information

CAS. Nr. 3077715-58-0
Appearance Solid
Molecular Weight 583.07
Formel C₃₄H₃₁ClN₂O₅
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
Versand

Room temperature in continental US; may vary elsewhere.
Speicherung

4°C, protect from light

* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)

Lösungsmittel & Löslichkeit

In Vitro:

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)

View the Complete Stock Solution Preparation Table

Preparing Stock Solutions

View the Complete Stock Solution Preparation Table

Concentration Solvent Mass

1 mg

5 mg

10 mg

Concentration

Solvent

Mass

1 mM

1.7151 mL

8.5753 mL

17.1506 mL

5 mM

0.3430 mL

1.7151 mL

3.4301 mL

10 mM

0.1715 mL

0.8575 mL

1.7151 mL

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.

Molaritätsrechner

Mass (g) = Concentration (mol/L) × Volume (L) × Molecular Weight (g/mol)

Mass Mass

Konzentration Konzentration

Volumen Volumen

Molecular Weight Molecular Weight

Verdünnungsrechner

Konzentration _{(Stammlösung)} × Volumen _{(Stammlösung)} = Konzentration _{(Ziellösung)} × Volumen _{(Ziellösung)}

Konzentration _{(Stammlösung)} Konzentration _{(Stammlösung)}

Volumen _{(Stammlösung)} Volumen _{(Stammlösung)}

Konzentration _{(Ziellösung)} Konzentration _{(Ziellösung)}

Volumen _{(Ziellösung)} Volumen _{(Ziellösung)}

In Vivo:

Select the appropriate dissolution method based on your experimental animal and administration route.

Stock Solution Working Solution

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.

Protocol 1

Add each solvent one by one: 10% DMSO 90% Corn Oil

Solubility: 5 mg/mL (8.58 mM); Clear solution; Need ultrasonic

This protocol yields a clear solution of 5 mg/mL. If the continuous dosing period exceeds half a month, please choose this protocol carefully.

Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (50.0 mg/mL) to 900 μL Corn oil, and mix evenly.

In Vivo Dissolution Calculator

Please enter the basic information of animal experiments:

Dosage Dosage
mg/kg
Animal Weight (Per Animal) Animal Weight (Per Animal)
g
Dosing Volume (Per Animal) Dosing Volume (Per Animal)
μL
Number of Animals Number of Animals

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Recommended: Prepare an additional quantity of animals to account for potential losses during experiments.

Please enter your animal formula composition:

%
DMSO +

Recommended: Keep the proportion of DMSO in working solution below 2% if your animal is weak.
%
+
+
%
Tween-80 + +
%
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

Reinheit & Dokumentation

Select Batch:

Reinheit: 99.98%

Assay: 99.98%

ee.: 99.98%

Data Sheet (271 KB)
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)
COA (2659 KB)
Elemental Analysis Report (2659 KB)
HNMR (2659 KB)
CNMR (2659 KB)
RP-HPLC (2659 KB)
NP-HPLC (2659 KB)
MS (2659 KB)
LCMS (2659 KB)
IR (2659 KB)
GC (2659 KB)
OR (2659 KB)
SDS-PAGE (2659 KB)
SEC-HPLC (2659 KB)
Other Report (2659 KB)
Handling Instructions (2659 KB)

Verweise

[1]. Xia A, et al. Cryo-EM structures of human GPR34 enable the identification of selective antagonists. Proc Natl Acad Sci U S A. 2023;120(39):e2308435120. [Content Brief]

Help & FAQs

How should lyophilized recombinant proteins be reconstituted and stored?

1. Before opening the cap, centrifuge the vial at 13000 rpm for 20-30 seconds. This step will ensure that any lyophilized powder that may have adhered to the cap or walls is collected at the bottom of the vial, minimizing the risk of product loss.

Complete Stock Solution Preparation Table

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

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YL-365

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Anti-Pulmonary Fibrosis Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

YL-365

GPCR/G Protein Compound Library

Immunology/Inflammation Compound Library

Anti-Pulmonary Fibrosis Compound Library

Highly Selective Inhibitors Library

Bioactive Compound Library Max

MCE Bioactive Compound Library

Bioactive Compound Library

High-Throughput Bioactive Compound Library

Lactylation Compound Library

Biologische Aktivität

Chemical Information

Lösungsmittel & Löslichkeit

Reinheit & Dokumentation

Verweise

Help & FAQs

Complete Stock Solution Preparation Table

YL-365 Related Classifications

HY-156815 Related Classifications