Synonym
SR7826; SR-7826; SR 7826;
IUPAC/Chemical Name
1-(2-Hydroxy-ethyl)-3-[4-(5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl)-phenyl]-1-phenyl-urea
InChi Key
WQAGVQVBDHOHRD-UHFFFAOYSA-N
InChi Code
InChI=1S/C22H21N5O2/c1-15-13-23-21-19(15)20(24-14-25-21)16-7-9-17(10-8-16)26-22(29)27(11-12-28)18-5-3-2-4-6-18/h2-10,13-14,28H,11-12H2,1H3,(H,26,29)(H,23,24,25)
SMILES Code
O=C(NC1=CC=C(C2=C3C(NC=C3C)=NC=N2)C=C1)N(CCO)C4=CC=CC=C4
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
>3 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
2934.99.03.00
Biological target:
SR7826 is a LIMK inhibitor (IC50 values are 43, 5536 and 6565 nM for LIMK1, ROCKI and ROCKII, respectively).
In vitro activity:
SR7826 inhibited contractions of prostate strips, which were induced by electrical field stimulation, α1 -adrenoceptor agonists phenylephrine and methoxamine and the TXA2 analogue, U46619. In WPMY-1 cells, SR7826 caused breakdown of actin filaments and reduced viability.
Reference: Br J Pharmacol. 2018 Jun;175(11):2077-2096. https://pubmed.ncbi.nlm.nih.gov/29574791/
In vivo activity:
LIMK inhibitors, such as SR7826, could be a potential therapeutic strategy for overactive bladder- related lower urinary tract symptoms. Treatment with SR7826 or LIMKi3 decreased micturition frequency and bladder detrusor hypertrophy in rats with bladder outlet obstruction.
Reference: Acta Pharm Sin B. 2021 Jul;11(7):1914-1930. https://pubmed.ncbi.nlm.nih.gov/34386328/
|
Solvent |
mg/mL |
mM |
comments |
Solubility |
DMSO |
38.7 |
100.00 |
|
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
387.44
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 |
Formulation protocol:
1. Yu Q, Gratzke C, Wang Y, Herlemann A, Sterr CM, Rutz B, Ciotkowska A, Wang X, Strittmatter F, Stief CG, Hennenberg M. Inhibition of human prostate smooth muscle contraction by the LIM kinase inhibitors, SR7826 and LIMKi3. Br J Pharmacol. 2018 Jun;175(11):2077-2096. doi: 10.1111/bph.14201. Epub 2018 Apr 29. PMID: 29574791; PMCID: PMC5978953.
2. Yu Q, Wu C, Chen Y, Li B, Wang R, Huang R, Li X, Gu D, Wang X, Duan X, Li S, Liu Y, Wu W, Hennenberg M, Zeng G. Inhibition of LIM kinase reduces contraction and proliferation in bladder smooth muscle. Acta Pharm Sin B. 2021 Jul;11(7):1914-1930. doi: 10.1016/j.apsb.2021.01.005. Epub 2021 Jan 7. PMID: 34386328; PMCID: PMC8343115.
In vitro protocol:
1. Yu Q, Gratzke C, Wang Y, Herlemann A, Sterr CM, Rutz B, Ciotkowska A, Wang X, Strittmatter F, Stief CG, Hennenberg M. Inhibition of human prostate smooth muscle contraction by the LIM kinase inhibitors, SR7826 and LIMKi3. Br J Pharmacol. 2018 Jun;175(11):2077-2096. doi: 10.1111/bph.14201. Epub 2018 Apr 29. PMID: 29574791; PMCID: PMC5978953.
In vivo protocol:
1. Yu Q, Wu C, Chen Y, Li B, Wang R, Huang R, Li X, Gu D, Wang X, Duan X, Li S, Liu Y, Wu W, Hennenberg M, Zeng G. Inhibition of LIM kinase reduces contraction and proliferation in bladder smooth muscle. Acta Pharm Sin B. 2021 Jul;11(7):1914-1930. doi: 10.1016/j.apsb.2021.01.005. Epub 2021 Jan 7. PMID: 34386328; PMCID: PMC8343115.
1: Yu Q, Gratzke C, Wang Y, Herlemann A, Sterr CM, Rutz B, Ciotkowska A, Wang X, Strittmatter F, Stief CG, Hennenberg M. Inhibition of human prostate smooth muscle contraction by the LIM kinase inhibitors, SR7826 and LIMKi3. Br J Pharmacol. 2018 Jun;175(11):2077-2096. doi: 10.1111/bph.14201. Epub 2018 Apr 29. PubMed PMID: 29574791; PubMed Central PMCID: PMC5978953.
2: Yu Q, Wu C, Chen Y, Li B, Wang R, Huang R, Li X, Gu D, Wang X, Duan X, Li S, Liu Y, Wu W, Hennenberg M, Zeng G. Inhibition of LIM kinase reduces contraction and proliferation in bladder smooth muscle. Acta Pharm Sin B. 2021 Jul;11(7):1914-1930. doi: 10.1016/j.apsb.2021.01.005. Epub 2021 Jan 7. PMID: 34386328; PMCID: PMC8343115.