GR 64349
Based on 1 Customer Validation
GR 64349 is a selective neurokinin 2 (NK2) receptor agonist. GR 64349 selectively activates the NK-2 receptor subtype. GR 64349 activates tonic and rhythmic bladder contractions of the micturition reflex. GR 64349 acetate does not inhibit rhythmic bladder contraction activation induced by normal saline. GR 64349 induces inward currents.
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- Pureza : 99.45%
- No. CAS: 137593-52-3
- Fòrmula: C42H68N10O11S
- Peso molecular:921.11
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Almacenamiento:
Sealed storage, away from moisture.
Powder -80°C, 2 years , -20°C, 1 year* In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
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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Actividad biológica
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Chemical Information
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Solvente y solubilidad
- Pureza y Documentación
- Referencias
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Help & FAQs
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Actividad biológica
Descripciòn
IC50 & Target
[1]|
NK2R |
In Vitro
GR 64349 contracts isolated rat bladder tissues in vitro, with potency comparable to that of the selective NK-1 agonist GR 73632 (HY-P1192)[1].
GR 64349 (300-500 nM) generates inward currents in some neurons[2].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only. .
In Vivo
GR 64349 (intracerebroventricular injection) does not modulate centrally mediated rhythmic bladder contractions in urethane-anesthetized rats[1].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
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Animal Model:Wistar-Morini (male, 300-350 g, urethane-anesthetized, urinary bladder cannulated and filled to 0.25 mL saline)[1]
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Dosage:0.1 nmoles/kg; 1 nmoles/kg; 10 nmoles/kg
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Administration:i.a.
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Result:Induced a dose-related increase in intravesical pressure (tonic contraction, TC) and activation of rhythmic bladder contractions (RBC).
Reached maximal TC amplitude of 37 mmHg (n=6-7).
Achieved ED50 of 0.61 nmoles/kg i.a. for TC (95% confidence limits: 0.36-1.03).
Achieved ED50 of 0.43 nmoles/kg i.a. for RBC (95% confidence limits: 0.15-1.26).
Observed RBC in 4-6 out of 6 preparations at 1 nmoles/kg i.a.
Left TC largely unaffected after topical TTX pretreatment, which abolished RBC.
Showed maximal TC amplitudes of 28 mmHg (without antagonist) and 26 mmHg (with GR 82334 pretreatment, n=5), with GR 82334 not inhibiting GR 64349-induced TC.
Chemical Information
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No. CAS 137593-52-3
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Appearance Solid
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Peso molecular 921.11
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Fòrmula C42H68N10O11S
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Color White to off-white
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Sequence
Lys-Asp-Ser-Phe-Val-{Aaa}-Leu-Met-NH2
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Sequence Shortening
KDSFV{Aaa}LM-NH2
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Envío
Room temperature in continental US; may vary elsewhere.
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Almacenamiento
Sealed storage, away from moisture
Powder -80°C 2 years -20°C 1 year * In solvent : -80°C, 6 months; -20°C, 1 month (sealed storage, away from moisture)
Solvente y solubilidad
In Vitro:
H2O : ≥ 50 mg/mL (54.28 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). 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). 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)
Pureza y Documentación
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Ficha de datos (274 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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Instrucciones de manejo (2659 KB)
Referencias
[1]. Palea S, et al. Further studies on the effects of selective neurokinin agonists upon the activation of micturition reflex in rats. Evidence for a dual NK-1 receptor mediated excitatory and inhibitory activity. Neuropeptides. 1993 May;24(5):285-91. [Content Brief]
[2]. Drew GM, et al. Postsynaptic actions of substance P on rat periaqueductal grey neurons in vitro. Neuropharmacology. 2005;49(5):587-595. [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). 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 | 1 mM | 1.0856 mL | 5.4282 mL | 10.8565 mL | 27.1412 mL |
| 5 mM | 0.2171 mL | 1.0856 mL | 2.1713 mL | 5.4282 mL | |
| 10 mM | 0.1086 mL | 0.5428 mL | 1.0856 mL | 2.7141 mL | |
| 15 mM | 0.0724 mL | 0.3619 mL | 0.7238 mL | 1.8094 mL | |
| 20 mM | 0.0543 mL | 0.2714 mL | 0.5428 mL | 1.3571 mL | |
| 25 mM | 0.0434 mL | 0.2171 mL | 0.4343 mL | 1.0856 mL | |
| 30 mM | 0.0362 mL | 0.1809 mL | 0.3619 mL | 0.9047 mL | |
| 40 mM | 0.0271 mL | 0.1357 mL | 0.2714 mL | 0.6785 mL | |
| 50 mM | 0.0217 mL | 0.1086 mL | 0.2171 mL | 0.5428 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.
GR 64349 Related Classifications
HY-P1278 Related Classifications
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