WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 581164
CAS#: 219311-44-1 (free base)
Description: Dabuzalgron (previously codenamed R-450; Ro-115-1240) is a novel partial alphaA/IL receptor agonist that is administered in its hydrochloride form to control urethral smooth muscle contraction. The hemodynamic changes in the drug are very small and it is a potential drug for the treatment of stress urinary incontinence.
MedKoo Cat#: 581164
CAS#: 219311-44-1 (free base)
Chemical Formula: C12H16ClN3O3S
Exact Mass: 317.0601
Molecular Weight: 317.79
Elemental Analysis: C, 45.35; H, 5.08; Cl, 11.16; N, 13.22; O, 15.10; S, 10.09
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Synonym: Dabuzalgron; UNII-LGX4GZ74WO; R-450; Ro-115-1240;
IUPAC/Chemical Name: N-(6-Chloro-3-((4,5-dihydro-1H-imidazol-2-yl)methoxy)-2-methylphenyl)methanesulfonamide
InChi Key: FOYWMEJSRSBQGB-UHFFFAOYSA-N
InChi Code: InChI=1S/C12H16ClN3O3S/c1-8-10(19-7-11-14-5-6-15-11)4-3-9(13)12(8)16-20(2,17)18/h3-4,16H,5-7H2,1-2H3,(H,14,15)
SMILES Code: CS(=O)(NC1=C(Cl)C=CC(OCC2=NCCN2)=C1C)=O
Appearance: Solid powder
Purity: >98% (or refer to the Certificate of Analysis)
Shipping Condition: Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition: Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility: Soluble in DMSO
Shelf Life: >2 years if stored properly
Drug Formulation: This drug may be formulated in DMSO
Stock Solution Storage: 0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code: 2934.99.9001
The following data is based on the product molecular weight 317.79 Batch specific molecular weights may vary from batch to batch due to the degree of hydration, which will affect the solvent volumes required to prepare stock solutions.
|Concentration / Solvent Volume / Mass||1 mg||5 mg||10 mg|
|1 mM||1.15 mL||5.76 mL||11.51 mL|
|5 mM||0.23 mL||1.15 mL||2.3 mL|
|10 mM||0.12 mL||0.58 mL||1.15 mL|
|50 mM||0.02 mL||0.12 mL||0.23 mL|
1: Conlon K, Christy C, Westbrook S, Whitlock G, Roberts L, Stobie A, McMurray G. Pharmacological properties of 2-((R-5-chloro-4-methoxymethylindan-1-yl)-1H-imidazole (PF-3774076), a novel and selective alpha1A-adrenergic partial agonist, in in vitro and in vivo models of urethral function. J Pharmacol Exp Ther. 2009 Sep;330(3):892-901. doi: 10.1124/jpet.109.154963. Epub 2009 Jun 4. PubMed PMID: 19498105.
2: Musselman DM, Ford AP, Gennevois DJ, Harbison ML, Laurent AL, Mokatrin AS, Stoltz RR, Blue DR. A randomized crossover study to evaluate Ro 115-1240, a selective alpha1A/1L-adrenoceptor partial agonist in women with stress urinary incontinence. BJU Int. 2004 Jan;93(1):78-83. PubMed PMID: 14678373.
3: Wein AJ. A randomized crossover study to evaluate RO 115-1240, a selective alpha1A/1L-adrenoceptor partial agonist in women with stress urinary incontinence. BJU Int. 2004 Jun;93(9):1361. PubMed PMID: 15180647.
4: Wein AJ. A randomized crossover study to evaluate Ro 115-1240, a selective alpha-adrenoceptor partial agonist in women with stress urinary incontinence. BJU Int. 2004 May;93(7):1115. PubMed PMID: 15142177.
5: Blue DR, Daniels DV, Gever JR, Jett MF, O'Yang C, Tang HM, Williams TJ, Ford AP. Pharmacological characteristics of Ro 115-1240, a selective alpha1A/1L-adrenoceptor partial agonist: a potential therapy for stress urinary incontinence. BJU Int. 2004 Jan;93(1):162-70. PubMed PMID: 14678390.
6: Bayés M, Rabasseda X, Prous JR. Gateways to clinical trials. Methods Find Exp Clin Pharmacol. 2004 Apr;26(3):211-44. PubMed PMID: 15148527.
7: Beak J, Huang W, Parker JS, Hicks ST, Patterson C, Simpson PC, Ma A, Jin J, Jensen BC. An Oral Selective Alpha-1A Adrenergic Receptor Agonist Prevents Doxorubicin Cardiotoxicity. JACC Basic Transl Sci. 2017 Feb;2(1):39-53. doi: 10.1016/j.jacbts.2016.10.006. PubMed PMID: 28286875; PubMed Central PMCID: PMC5343290.