Upidosin
Based on 1 Customer Validation
Upidosin (Rec 15/2739) is an α-1 adrenoceptor (α-1 AR) antagonist. Upidosin shows moderate selectivity for the α-1A AR subtype. Upidosin shows uroselectivity in urethra and prostate with a Kb value of 2-3 nM higher than in ear artery and aorta with a Kb value of 20-100 nM. Upidosin inhibits [3H]prazosin binding to cloned human α-1A adrenergic receptor. Upidosin can be used for the research of urethral obstruction.
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- Purity: 99.48%
- CAS No.: 152735-23-4
- 화학식: C31H33N3O4
- 분자량:511.61
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보관:
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
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Biological Activity
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Chemical Information
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용액&용해도
- 순도&문서
- References
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Biological Activity
Upidosin is one of the most potent compounds action on the prostate with comparing the apparent pKB values, but its potency is slightly lower than that of tamsulosin and is higher than the potencies of prazosin, terazosin and 5-methylurapidil[2]. Upidosin shows binding affinities to cloned humanα1A, humanα1B, humanα1D adrenoceptors with pKi value of 9.0, 7.5 and 8.6, respectively[3].
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
MedChemExpress (MCE) has not independently confirmed the accuracy of these methods. They are for reference only.
Chemical Information
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CAS No. 152735-23-4
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Appearance Solid
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분자량 511.61
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화학식 C31H33N3O4
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Color White to off-white
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SMILES
COC(C=CC=C1)=C1N(CC2)CCN2CCCNC(C3=C4C(C(C(C)=C(C5=CC=CC=C5)O4)=O)=CC=C3)=O
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Synonyms
Rec 15/2739; Recordati 15/2739; SB 216469
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선적
Room temperature in continental US; may vary elsewhere.
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보관
4°C, protect from light
* In solvent : -80°C, 6 months; -20°C, 1 month (protect from light)
용액&용해도
DMSO : 250 mg/mL (488.65 mM; Need ultrasonic; Hygroscopic DMSO has a significant impact on the solubility of product, please use newly opened DMSO)
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
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 (protect from light). When stored at -80°C, please use it within 6 months. When stored at -20°C, please use it within 1 month.
Concentration (start) × Volume (start) = Concentration (final) × Volume (final)
순도&문서
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Data Sheet (272 KB)
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SDS (252 KB)
- English - EN (252 KB)
- Français - FR (252 KB)
- Deutsch - DE (252 KB)
- Norwegian - NO (252 KB)
- Español - ES (252 KB)
- Swedish - SV (252 KB)
- Italian - IT (252 KB)
- Korean - KR (252 KB)
- Portuguese - PT (252 KB)
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Handling Instructions (2659 KB)
References
[1]. Leonardi A, et al. Pharmacological characterization of the uroselective alpha-1 antagonist Rec 15/2739 (SB 216469): role of the alpha-1L adrenoceptor in tissue selectivity, part I. J Pharmacol Exp Ther. 1997 Jun;281(3):1272-83. [Content Brief]
[2]. Testa R, et al. Functional antagonistic activity of Rec 15/2739, a novel alpha-1 antagonist selective for the lower urinary tract, on noradrenaline-induced contraction of human prostate and mesenteric artery. J Pharmacol Exp Ther. 1996 Jun;277(3):1237-46. [Content Brief]
[3]. Kenny BA, et al. Evaluation of the pharmacological selectivity profile of alpha 1 adrenoceptor antagonists at prostatic alpha 1 adrenoceptors: binding, functional and in vivo studies. Br J Pharmacol. 1996 Jun;118(4):871-8. [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 (protect from light). 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 |
|---|---|---|---|---|---|
| DMSO | 1 mM | 1.9546 mL | 9.7731 mL | 19.5461 mL | 48.8653 mL |
| 5 mM | 0.3909 mL | 1.9546 mL | 3.9092 mL | 9.7731 mL | |
| 10 mM | 0.1955 mL | 0.9773 mL | 1.9546 mL | 4.8865 mL | |
| 15 mM | 0.1303 mL | 0.6515 mL | 1.3031 mL | 3.2577 mL | |
| 20 mM | 0.0977 mL | 0.4887 mL | 0.9773 mL | 2.4433 mL | |
| 25 mM | 0.0782 mL | 0.3909 mL | 0.7818 mL | 1.9546 mL | |
| 30 mM | 0.0652 mL | 0.3258 mL | 0.6515 mL | 1.6288 mL | |
| 40 mM | 0.0489 mL | 0.2443 mL | 0.4887 mL | 1.2216 mL | |
| 50 mM | 0.0391 mL | 0.1955 mL | 0.3909 mL | 0.9773 mL | |
| 60 mM | 0.0326 mL | 0.1629 mL | 0.3258 mL | 0.8144 mL | |
| 80 mM | 0.0244 mL | 0.1222 mL | 0.2443 mL | 0.6108 mL | |
| 100 mM | 0.0195 mL | 0.0977 mL | 0.1955 mL | 0.4887 mL |
Upidosin Related Classifications
HY-106954 Related Classifications
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