M871
Based on 1 Customer Validation
M871 (Galanin-(2-13)-Glu-His-(Pro)3-(Ala-Leu)2-Ala-amide) is an orally active and selective galanin receptor type 2 (GalR2) antagonist. M871 exhibits Ki values of 13.1 nM, 420 nM and >10 μM for GalR2, GalR1 and GalR3 respectively. M871 relieves the mice allergic rhinitis by reducing IgE production, as well as the number of B cells in tissues. M871 can inhibit the nerve invasion of salivary adenoid cystic carcinoma (SACC) and alleviate myocardial ischemia-reperfusion injury. M871 can be used for research on GalR2-related diseases (such as epilepsy, pain).
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- Pureté: 99.98%
- CAS No.: 908844-75-7
- Formule: C108H163N27O28
- Masse moléculaire:2287.61
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Stockage:
Sealed storage, away from moisture and light.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and 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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Activité biologique
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Chemical Information
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Solvant et solubilité
- Pureté et documentation
- Références
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Help & FAQs
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Activité biologique
GalR2[1].
M871 (10-8 M, 60 min) exhibits antagonist actions at galanin receptor type 2, blocking increased release of inositol phosphate produced by galanin in CHO cells[1].
M871 decreases SACC-83 cell invasion and migration to the dorsal root ganglia (DRG), as well as the growth and extension of neurites[5].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
M871 (3-12 mg/kg, i.v., single dose) protects the rat heart from ischemia/reperfusion (I/R) damage by a GalR2-dependent pathway[4].
M871 (p.o., once every third day for 4 weeks) significantly reduces tumor growth induced by SACC cells and the incidence of perineural invasion (PNI) in BALB/c mice[5].
M871 (4.575 mg/mL, bilateral intra-NAc injection, single dose) attenuates the Galanin (HY-P74132)-induced analgesic effect of inflammatory pain rats by activating CaMKII and PKC in nucleus accumbens (NAc) of inflammatory pain rats[6].
M871 (100 nM/kg, intracerebroventricular injection, once daily for 21 days) exacerbates hyperglycemia and aggravates the inflammatory response in type 2 diabetic rats[7].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:AR model established in six-week-old female BALB/c mice[3]
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Dosage:0.1 mg/kg
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Administration:Intranasal administration, once daily for 6 days
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Result:Increased levels of IL-4, IL-5, IL-6, IL-13, mKC and MIP2 and decreased IFN-γ.
Observed no significant differences in IFN-γ, IL-4, IL-5, IL-6, IL-13, mKC, MIP-2, TNF-a, IL-17, IL-25, or IL-33 levels between the AR.
Did not effectively suppress histamine-induced sneezing at all time points.
Suppressed an increase in IgE production and the number of nasal B cells induced during allergy.
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Animal Model:Myocardial I/R injury model established in male Wistar rats weighing 310 g[4]
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Dosage:3, 6, 8 and 12 mg/kg alone or 8 mg/kg with G1 (a pharmacological peptide agonist) /G2 (a full-length rat galanin)
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Administration:Intravenous injection (i.v.), single dose before 5 min before the onset of reperfusion
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Result:No effect of the coadministration with G1 or G2 on hemodynamic parameters compared with those after injection of G1 and G2 alone.
Did not increase the necrotic damage of the re-perfused heart by increasing doses from 3 to 8 mg/kg.
Completely blocked the protective effect of G1 and partially inhibited the protective effect of G2.
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Animal Model:Carrageenan-induced inflammatory pain model established in male Sprague-Dawley rats weighing 180-250 g[6]
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Dosage:4.575 mg/mL, dissolved in 1 µL of 6% acetonitrile
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Administration:Bilateral intra-NAc injection, single dose
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Result:Attenuated the Galanin-induced analgesic effect in NAc of inflammatory pain rats.
Reversed the M1145 (HY-P1135)-induced increases in HWL and HWT in NAc of inflammatory pain rats.
Significantly downregulated the expressions of p-CaMKII and p-PKC, but the levels of t-PKC and t-CaMKII were not significantly different.
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Animal Model:Type 2 diabetes model established in male Wistar rats[7]
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Dosage:100 nM/kg
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Administration:Intracerebroventricularly injection, once daily for 21 days
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Result:Displayed a significant increase in the plasma IL-1, IL-6, IL-8 and TNF-α, but an decrease in the plasma IL-22 and irisin compared with diabetic control rats.
Led to an enhancement in fasting glucose and decreased the glucose infusion rate.
Displayed a marked reduction in levels of GLUT4 and PGC-1α of skeletal muscles and adipocytes.
Chemical Information
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CAS No. 908844-75-7
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Appearance Solid
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Masse moléculaire 2287.61
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Formule C108H163N27O28
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Color White to off-white
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Synonyms
Galanin-(2-13)-Glu-His-(Pro)3-(Ala-Leu)2-Ala-amide
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Sequence
H2N-Trp-Thr-Leu-Asn-Ser-Ala-Gly-Tyr-Leu-Leu-Gly-Pro-Glu-His-Pro-Pro-Pro-Ala-Leu-Ala-Leu-Ala-NH2
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Sequence Shortening
WTLNSAGYLLGPEHPPPALALA-NH2
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Livraison
Room temperature in continental US; may vary elsewhere.
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Stockage
Sealed storage, away from moisture and light
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture and light)
Solvant et solubilité
DMSO : 100 mg/mL (43.71 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 (sealed storage, away from moisture and 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 (sealed storage, away from moisture and 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.
Add each solvent one by one: 10% DMSO 40% PEG300 5% Tween-80 45% Saline
Solubility: ≥ 2.5 mg/mL (1.09 mM); Clear solution
This protocol yields a clear solution of ≥ 2.5 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (25.0 mg/mL) to 400 μL PEG300, and mix evenly; then add 50 μL Tween-80 and mix evenly; then add 450 μL Saline to adjust the volume to 1 mL.
Preparation of Saline: Dissolve 0.9 g sodium chloride in ddH₂O and dilute to 100 mL to obtain a clear Saline solution.
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 (sealed storage, away from moisture and 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.
Pureté et documentation
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Fiche technique (278 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Instruction de manipulation (2659 KB)
Références
[3]. Kawada M, Yokoi H, Kimura T, Matsumoto Y, Sakurai H, Matsumoto K, Fujiwara M, Saito K. Involvement of galanin and galanin receptor 2 in a mouse model of allergic rhinitis. Allergol Int. 2022 Jan;71(1):83-93. [Content Brief]
[4]. Serebryakova L, et al. Exogenous GalR2-specific peptide agonist as a tool for treating myocardial ischemia/reperfusion injury. Fundam Clin Pharmacol. 2023 Dec;37(6):1109-1118. [Content Brief]
[5]. Wang J, et al. The GAL/GALR2 axis promotes the perineural invasion of salivary adenoid cystic carcinoma via epithelial-to-mesenchymal transition. Cancer Med. 2023 Feb;12(4):4496-4509. [Content Brief]
[6]. Li M, et al. Galanin Receptor 2 Is Involved in Galanin-Induced Analgesic Effect by Activating PKC and CaMKII in the Nucleus Accumbens of Inflammatory Pain Rats. Front Neurosci. 2021 Jan 21;14:593331. [Content Brief]
[7]. Fang P, et al. Central galanin receptor 2 mediates galanin action to promote systemic glucose metabolism of type 2 diabetic rats. Biochem Pharmacol. 2018 Oct;156:241-247. [Content Brief]
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 (sealed storage, away from moisture and 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 | 0.4371 mL | 2.1857 mL | 4.3714 mL | 10.9284 mL |
| 5 mM | 0.0874 mL | 0.4371 mL | 0.8743 mL | 2.1857 mL | |
| 10 mM | 0.0437 mL | 0.2186 mL | 0.4371 mL | 1.0928 mL | |
| 15 mM | 0.0291 mL | 0.1457 mL | 0.2914 mL | 0.7286 mL | |
| 20 mM | 0.0219 mL | 0.1093 mL | 0.2186 mL | 0.5464 mL | |
| 25 mM | 0.0175 mL | 0.0874 mL | 0.1749 mL | 0.4371 mL | |
| 30 mM | 0.0146 mL | 0.0729 mL | 0.1457 mL | 0.3643 mL | |
| 40 mM | 0.0109 mL | 0.0546 mL | 0.1093 mL | 0.2732 mL |
M871 Related Classifications
HY-P1130 Related Classifications
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