Bremelanotide Acetate
Based on 1 publication(s) in Google Scholar
Bremelanotide (PT-141) Acetate is a melanocortin receptor agonist. Bremelanotide Acetate can activate MC4R and increases dopamine release. Bremelanotide Acetate induces appetitive sexual behaviors, female mounting behavior, and repetitive self-grooming. Bremelanotide Acetate can be used for the research of hypoactive sexual desire disorders.
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- Pureté : 99.94%
- CAS No.: 1607799-13-2
- Formule: C52H72N14O12
- Masse moléculaire:1085.22
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Stockage:
Sealed storage, away from moisture and light, under nitrogen.
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, under nitrogen)
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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HY-N2466
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Publications Citing Use of MedChemExpress (MCE) Bremelanotide Acetate
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Activité biologique
Description
IC50 & Target
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MC3R |
MC4R |
In Vitro
Bremelanotide (10−3-105 nM) Acetate binds to MC3R and MC4R in a concentration-dependent manner[3].
Bremelanotide Acetate induces cAMP accumulation in cell-free assays with EC50 values of 0.4 nM for MC3R and 0.2 nM for MC4R[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
Bremelanotide (0.01-10 mg/kg; i.p.; single dose) Acetate induces dose-dependent repetitive grooming behavior in male and female mice, with 1 mg/kg being the lowest effective grooming dose that does not cause anxiety-like behavior[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Female rats (ovariectomized, hormone-primed with estradiol and progesterone, or estradiol alone)[1]
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Dosage:50, 100, 200 μg/kg
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Administration:Subcutaneously injection
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Result:Increased solicitations in estradiol + progesterone-primed rats at 100 and 200 μg/kg.
Increased solicitations in estradiol-alone primed rats at 200 μg/kg.
Increased hops and darts in estradiol + progesterone-primed rats at 100 and 200 μg/kg.
Induced female mounting behavior at 200 μg/kg.
Essai clinique
| NCT Number | Sponsor | Condition | Start Date |
Phase
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|---|---|---|---|---|
| NCT01329991 | Plexxikon| | 2011-05 | PHASE1 |
Chemical Information
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CAS No. 1607799-13-2
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Appearance Solid
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Masse moléculaire 1085.22
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Formule C52H72N14O12
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Color White to off-white
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Synonyms
PT-141 Acetate
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Sequence
Ac-[Nle}-Asp-His-{d-Phe}-Arg-Trp-Lys (Lactam bridge: Asp4-Lys7)
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Sequence Shortening
Ac-[Nle}-DHFRWK (Lactam bridge: Asp4-Lys7)
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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, under nitrogen
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, under nitrogen)
Publications (1)
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Journal Impact Factor
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Most Recent
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Mol Pharm
2022 Nov 7;19(11):4320-4332. PMID: 36269563
Solvant et solubilité
In Vitro:
DMSO : 100 mg/mL (92.15 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
H2O : ≥ 50 mg/mL (46.07 mM)
* "≥" means soluble, but saturation unknown.
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, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
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, under nitrogen). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
In Vivo:
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: ≥ 2.08 mg/mL (1.92 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 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.
Add each solvent one by one: 10% DMSO 90% (20% SBE-β-CD in Saline)
Solubility: ≥ 2.08 mg/mL (1.92 mM); Clear solution
This protocol yields a clear solution of ≥ 2.08 mg/mL (saturation unknown).
Taking 1 mL working solution as an example, add 100 μL DMSO stock solution (20.8 mg/mL) to 900 μL 20% SBE-β-CD in Saline, and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C, storage for one week): 2 g SBE-β-CD powder is dissolved in 10 mL Saline, completely dissolve until clear.
In Vivo Dissolution Calculator
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.
Working solution concentration: 0.22 mg/mL
This product has good water solubility, please refer to the measured solubility data in water/PBS/Saline for details.
Pureté et documentation
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Fiche technique (281 KB)
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SDS (254 KB)
- English - EN (254 KB)
- Français - FR (254 KB)
- Deutsch - DE (254 KB)
- Norwegian - NO (254 KB)
- Español - ES (254 KB)
- Swedish - SV (254 KB)
- Italian - IT (254 KB)
- Korean - KR (254 KB)
- Portuguese - PT (254 KB)
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Instruction de manipulation (2659 KB)
Références
[1]. Pfaus J, et al. Bremelanotide: an overview of preclinical CNS effects on female sexual function. J Sex Med. 2007;4 Suppl 4:269-279. [Content Brief]
[3]. Molinoff PB, et al. PT-141: a melanocortin agonist for the treatment of sexual dysfunction. Ann N Y Acad Sci. 2003 Jun;994:96-102. [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, under nitrogen). 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 |
|---|---|---|---|---|---|
| H2O / DMSO | 1 mM | 0.9215 mL | 4.6074 mL | 9.2147 mL | 23.0368 mL |
| 5 mM | 0.1843 mL | 0.9215 mL | 1.8429 mL | 4.6074 mL | |
| 10 mM | 0.0921 mL | 0.4607 mL | 0.9215 mL | 2.3037 mL | |
| 15 mM | 0.0614 mL | 0.3072 mL | 0.6143 mL | 1.5358 mL | |
| 20 mM | 0.0461 mL | 0.2304 mL | 0.4607 mL | 1.1518 mL | |
| 25 mM | 0.0369 mL | 0.1843 mL | 0.3686 mL | 0.9215 mL | |
| 30 mM | 0.0307 mL | 0.1536 mL | 0.3072 mL | 0.7679 mL | |
| 40 mM | 0.0230 mL | 0.1152 mL | 0.2304 mL | 0.5759 mL | |
| DMSO | 50 mM | 0.0184 mL | 0.0921 mL | 0.1843 mL | 0.4607 mL |
| 60 mM | 0.0154 mL | 0.0768 mL | 0.1536 mL | 0.3839 mL | |
| 80 mM | 0.0115 mL | 0.0576 mL | 0.1152 mL | 0.2880 mL |
* Note: If you choose water as the stock solution, please dilute it to the working solution, then filter and sterilize it with a 0.22 μm filter before use.
Bremelanotide Acetate Related Classifications
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