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GW438014A 469861-49-2

GW438014A 469861-49-2

CAS No.: 469861-49-2

GW438014A is a potent and specific NPY-Y5 receptor blocker (antagonist). GW438014A inhibits food intake and reduces weig
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This product is for research use only, not for human use. We do not sell to patients.

GW438014A is a potent and specific NPY-Y5 receptor blocker (antagonist). GW438014A inhibits food intake and reduces weight gain in obese rodents.

Physicochemical Properties


Molecular Formula C23H23N3O4S
Molecular Weight 437.511424303055
Exact Mass 341.152
CAS # 469861-49-2
PubChem CID 6918627
Appearance White to off-white solid powder
LogP 4.5
Hydrogen Bond Donor Count 1
Hydrogen Bond Acceptor Count 2
Rotatable Bond Count 5
Heavy Atom Count 26
Complexity 456
Defined Atom Stereocenter Count 0
SMILES

S(C)(=O)(=O)O.O=C(C1C=CC=CC=1)NC1=NC2C=CC=CC=2N1CCC1C=CC=CC=1

InChi Key CDUDZZGLFOFINU-UHFFFAOYSA-N
InChi Code

InChI=1S/C22H19N3O/c26-21(18-11-5-2-6-12-18)24-22-23-19-13-7-8-14-20(19)25(22)16-15-17-9-3-1-4-10-17/h1-14H,15-16H2,(H,23,24,26)
Chemical Name

N-[1-(2-phenylethyl)benzimidazol-2-yl]benzamide
Synonyms

GW 438014 A; GW-438014-A; GW438014A
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

Shipping Condition Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)

Biological Activity


ln Vivo In a genetically dynamic ob/ob paradigm of spontaneous and sleep-induced food gain, GW438014A (10 mg/kg; ip; daily, for 7 d) decreases food-induced and NPY-induced food intake [1].
Animal Protocol Animal/Disease Models: obese ob/ob mice [1]
Doses: 10 mg/kg
Route of Administration: intraperitoneal (ip) injection; one time/day for 7 days.
Experimental Results: The weight gain rate of lean rats and obese rats was diminished.
References

[1]. Food intake inhibition and reduction in body weight gain in lean and obese rodents treated with GW438014A, a potent and selective NPY-Y5 receptor antagonist. Regul Pept. 2002 Jun 15;106(1-3):47-54.


Solubility Data


Solubility (In Vitro) DMSO : ~250 mg/mL (~571.42 mM)
Solubility (In Vivo) Note: Listed below are some common formulations that may be used to formulate products with low water solubility (e.g. < 1 mg/mL), you may test these formulations using a minute amount of products to avoid loss of samples.

Injection Formulations
(e.g. IP/IV/IM/SC)
Injection Formulation 1: DMSO : Tween 80: Saline = 10 : 5 : 85 (i.e. 100 μL DMSO stock solution 50 μL Tween 80 850 μL Saline)
*Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH ₂ O to obtain a clear solution.
Injection Formulation 2: DMSO : PEG300 :Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL DMSO 400 μLPEG300 50 μL Tween 80 450 μL Saline)
Injection Formulation 3: DMSO : Corn oil = 10 : 90 (i.e. 100 μL DMSO 900 μL Corn oil)
Example: Take the Injection Formulation 3 (DMSO : Corn oil = 10 : 90) as an example, if 1 mL of 2.5 mg/mL working solution is to be prepared, you can take 100 μL 25 mg/mL DMSO stock solution and add to 900 μL corn oil, mix well to obtain a clear or suspension solution (2.5 mg/mL, ready for use in animals).
Injection Formulation 4: DMSO : 20% SBE-β-CD in saline = 10 : 90 [i.e. 100 μL DMSO 900 μL (20% SBE-β-CD in saline)]
*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.
Injection Formulation 5: 2-Hydroxypropyl-β-cyclodextrin : Saline = 50 : 50 (i.e. 500 μL 2-Hydroxypropyl-β-cyclodextrin 500 μL Saline)
Injection Formulation 6: DMSO : PEG300 : castor oil : Saline = 5 : 10 : 20 : 65 (i.e. 50 μL DMSO 100 μLPEG300 200 μL castor oil 650 μL Saline)
Injection Formulation 7: Ethanol : Cremophor : Saline = 10: 10 : 80 (i.e. 100 μL Ethanol 100 μL Cremophor 800 μL Saline)
Injection Formulation 8: Dissolve in Cremophor/Ethanol (50 : 50), then diluted by Saline
Injection Formulation 9: EtOH : Corn oil = 10 : 90 (i.e. 100 μL EtOH 900 μL Corn oil)
Injection Formulation 10: EtOH : PEG300:Tween 80 : Saline = 10 : 40 : 5 : 45 (i.e. 100 μL EtOH 400 μLPEG300 50 μL Tween 80 450 μL Saline)

Oral Formulations Oral Formulation 1: Suspend in 0.5% CMC Na (carboxymethylcellulose sodium)
Oral Formulation 2: Suspend in 0.5% Carboxymethyl cellulose
Example: Take the Oral Formulation 1 (Suspend in 0.5% CMC Na) as an example, if 100 mL of 2.5 mg/mL working solution is to be prepared, you can first prepare 0.5% CMC Na solution by measuring 0.5 g CMC Na and dissolve it in 100 mL ddH2O to obtain a clear solution; then add 250 mg of the product to 100 mL 0.5% CMC Na solution, to make the suspension solution (2.5 mg/mL, ready for use in animals).
Oral Formulation 3: Dissolved in PEG400
Oral Formulation 4: Suspend in 0.2% Carboxymethyl cellulose
Oral Formulation 5: Dissolve in 0.25% Tween 80 and 0.5% Carboxymethyl cellulose
Oral Formulation 6: Mixing with food powders

Note: Please be aware that the above formulations are for reference only. InvivoChem strongly recommends customers to read literature methods/protocols carefully before determining which formulation you should use for in vivo studies, as different compounds have different solubility properties and have to be formulated differently.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.2857 mL 11.4283 mL 22.8566 mL
5 mM 0.4571 mL 2.2857 mL 4.5713 mL
10 mM 0.2286 mL 1.1428 mL 2.2857 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.