WAY 207024 dihydrochlorideGnRH-R antagonist, potent CAS# 872002-73-8 |
Quality Control & MSDS
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| Cas No. | 872002-73-8 | SDF | Download SDF |
| PubChem ID | 69403574 | Appearance | Powder |
| Formula | C30H34Cl2N6 | M.Wt | 549.54 |
| Type of Compound | N/A | Storage | Desiccate at -20°C |
| Solubility | Soluble to 85 mM in DMSO | ||
| Chemical Name | 6-[[4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl]methyl]quinoxaline;dihydrochloride | ||
| SMILES | CC(C)(C)C1=CC=C(C=C1)C2=NC3=C(N2)C=CC=C3N4CCN(CC4)CC5=CC6=NC=CN=C6C=C5.Cl.Cl | ||
| Standard InChIKey | REQCNTGYEABOIT-UHFFFAOYSA-N | ||
| Standard InChI | InChI=1S/C30H32N6.2ClH/c1-30(2,3)23-10-8-22(9-11-23)29-33-25-5-4-6-27(28(25)34-29)36-17-15-35(16-18-36)20-21-7-12-24-26(19-21)32-14-13-31-24;;/h4-14,19H,15-18,20H2,1-3H3,(H,33,34);2*1H | ||
| General tips | For obtaining a higher solubility , please warm the tube at 37 ℃ and shake it in the ultrasonic bath for a while.Stock solution can be stored below -20℃ for several months. We recommend that you prepare and use the solution on the same day. However, if the test schedule requires, the stock solutions can be prepared in advance, and the stock solution must be sealed and stored below -20℃. In general, the stock solution can be kept for several months. Before use, we recommend that you leave the vial at room temperature for at least an hour before opening it. |
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| About Packaging | 1. The packaging of the product may be reversed during transportation, cause the high purity compounds to adhere to the neck or cap of the vial.Take the vail out of its packaging and shake gently until the compounds fall to the bottom of the vial. 2. For liquid products, please centrifuge at 500xg to gather the liquid to the bottom of the vial. 3. Try to avoid loss or contamination during the experiment. |
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| Shipping Condition | Packaging according to customer requirements(5mg, 10mg, 20mg and more). Ship via FedEx, DHL, UPS, EMS or other couriers with RT, or blue ice upon request. | ||
| Description | Gonadotropin releasing hormone receptor (GnRH-R) antagonist. Exhibits potent affinity (IC50 values are 12 and 71 nM for human and rat GnRH receptors respectively). Lowers plasma leuteinizing hormone levels in the rat. Orally active. |
WAY 207024 dihydrochloride Dilution Calculator
WAY 207024 dihydrochloride Molarity Calculator
| 1 mg | 5 mg | 10 mg | 20 mg | 25 mg | |
| 1 mM | 1.8197 mL | 9.0985 mL | 18.197 mL | 36.3941 mL | 45.4926 mL |
| 5 mM | 0.3639 mL | 1.8197 mL | 3.6394 mL | 7.2788 mL | 9.0985 mL |
| 10 mM | 0.182 mL | 0.9099 mL | 1.8197 mL | 3.6394 mL | 4.5493 mL |
| 50 mM | 0.0364 mL | 0.182 mL | 0.3639 mL | 0.7279 mL | 0.9099 mL |
| 100 mM | 0.0182 mL | 0.091 mL | 0.182 mL | 0.3639 mL | 0.4549 mL |
| * Note: If you are in the process of experiment, it's necessary to make the dilution ratios of the samples. The dilution data above is only for reference. Normally, it's can get a better solubility within lower of Concentrations. | |||||
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WAY 207024 dihydrochloride is a potent gonadotropin releasing hormone receptor (GnRH-R) antagonist with IC50 values of 12 and 71 nM for human and rat GnRH receptors, respectively [1].
GnRH-R is a member of the G-protein coupled receptor (GPCR) family. Activation of the receptor by binding of gonadotropin-releasing hormone causes the release of leuteinizing hormone (LH) and follicle stimulating hormone (FSH) from the anterior pituitary gland and they in turn stimulate sex hormone synthesis and release into the general circulation [1].
WAY 207024 dihydrochloride displayed moderate membrane permeability properties and rat liver microsome stability [1].
In castrated rats, WAY 207024 dihydrochloride was absorbed well following oral administration with a bioavailability of 74%. Also, WAY 207024 dihydrochloride (30 mg/kg, oral gavage) reduced serum LH levels starting at 1 h post dosing and LH levels had returned to the vehicle treated group levels after 24h [1].
References:
[1]. Pelletier JC, Chengalvala MV, Cottom JE, et al. Discovery of 6-({4-[2-(4-tert-butylphenyl)-1H-benzimidazol-4-yl]piperazin-1-yl}methyl)quinoxaline (WAY-207024): an orally active antagonist of the gonadotropin releasing hormone receptor (GnRH-R). J Med Chem, 2009, 52(7): 2148-2152.
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Design and synthesis of a cyclic double mutant peptide (cyclo(87-99)[A91,A96]MBP87-99) induces altered responses in mice after conjugation to mannan: implications in the immunotherapy of multiple sclerosis.[Pubmed:19072222]
J Med Chem. 2009 Jan 8;52(1):214-8.
Altered peptide ligands that alter immune responses are a promising approach to the immunotherapy of multiple sclerosis. Cyclic peptides are of interest because the limited stability of linear peptides restricts their use in vivo. We designed and synthesized a cyclic double mutant peptide from MBP(87-99)-[cyclo(87-99)[A(91),A(96)]MBP(87-99)]. Immunization of mice, in CFA reduced Th1 responses. However, when conjugated to reduced mannan, a significant further reduction of Th1 responses and moderate Th2 responses were induced.
