Size | Price | Stock | Qty |
---|---|---|---|
1mg |
|
||
5mg |
|
||
10mg |
|
||
50mg |
|
||
Other Sizes |
|
Targets |
MC4R
|
---|---|
ln Vitro |
With a mean IC50 of 0.32 μM, 0.81 μM, and 2.12 μM for hMC4-R, hMC3-R, and hMC5-R, respectively, ML-00253764 displaces NDP-α-MSH binding[1]. In HEK293 cell membranes expressing MC4R, ML-00253764 (100 μM) reduces cAMP synthesis by 20% when triggered by [NLE4,D-Phe7]-α-melanocyte stimulating hormone ([NDP]-α-MSH); however, it had no effect on cAMP levels in membranes expressing MC3R or MC5R[1].
|
ln Vivo |
Chronic peripheral dose of ML-00253764 (subcutaneous injection; 3, 10, or 30 mg/kg; once daily) protects against tumor-induced body weight loss in BALB/c mice harboring CT-26 tumors[1]. Polyethylene glycol 200/saline (1:10) dissolves ML-00253764 in a volume of 10 mL/kg (For reference only)[1].
|
Animal Protocol |
Animal/Disease Models: CT-26 tumor bearing BALB/c mice[1]
Doses: 3, 10 , or 30 mg/kg Route of Administration: subcutaneous (sc) injection; 3, 10, or 30 mg/kg; one time/day Experimental Results: decreased tumor-induced weight loss in a mouse model. |
References |
[1]. Vos TJ, et al. Identification of 2-[2-[2-(5-bromo-2- methoxyphenyl)-ethyl]-3-fluorophenyl]-4,5-dihydro-1H-imidazole (ML00253764), a small molecule melanocortin 4 receptor antagonist that effectively reduces tumor-induced weight loss in a mouse model. J Med Chem. 2004 Mar 25;47(7):1602-4.
|
Molecular Formula |
C18H19BRCLFN2O
|
---|---|
Molecular Weight |
413.71
|
CAS # |
1706524-94-8
|
Related CAS # |
ML00253764;681847-92-7
|
Appearance |
Typically exists as solids (or liquids in special cases) at room temperature
|
SMILES |
C(C1C(=CC=CC=1C1=NCCN1)F)CC1C=C(Br)C=CC=1OC.Cl
|
HS Tariff Code |
2934.99.9001
|
Storage |
Powder -20°C 3 years 4°C 2 years In solvent -80°C 6 months -20°C 1 month Note: Please store this product in a sealed and protected environment, avoid exposure to moisture. |
Shipping Condition |
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
|
Solubility (In Vitro) |
DMSO: 12.5 mg/mL (30.21 mM)
|
---|---|
Solubility (In Vivo) |
Solubility in Formulation 1: ≥ 1.25 mg/mL (3.02 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL. Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution. Solubility in Formulation 2: ≥ 1.25 mg/mL (3.02 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution. For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly. Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution. View More
Solubility in Formulation 3: ≥ 1.25 mg/mL (3.02 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution. |
Preparing Stock Solutions | 1 mg | 5 mg | 10 mg | |
1 mM | 2.4172 mL | 12.0858 mL | 24.1715 mL | |
5 mM | 0.4834 mL | 2.4172 mL | 4.8343 mL | |
10 mM | 0.2417 mL | 1.2086 mL | 2.4172 mL |
*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.
Calculation results
Working concentration: mg/mL;
Method for preparing DMSO stock solution: mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation::Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.
(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
(2) Be sure to add the solvent(s) in order.