{"product_id":"m33148","title":"SR7826","description":"\u003cp style=\"padding-left:1em;\"\u003eSR7826 is a class of bis-aryl urea derived potent, selective and orally active LIM kinase (LIMK) inhibitor with an IC50 of 43 nM for LIMK1. SR7826 is \u0026gt;100-fold more selective for LIMK1 than ROCK and JNK kinases.\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eProduct information\u003c\/strong\u003e\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eCAS Number:\u003c\/strong\u003e 1219728-20-7\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eMolecular Weight:\u003c\/strong\u003e 387.43\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eFormula:\u003c\/strong\u003e C22H21N5O2\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eChemical Name:\u003c\/strong\u003e 1-(2-hydroxyethyl)-3-(4-{5-methyl-7H-pyrrolo[2,3-d]pyrimidin-4-yl}phenyl)-1-phenylurea\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eSmiles:\u003c\/strong\u003e CC1=CNC2=NC=NC(=C21)C1C=CC(=CC=1)NC(=O)N(CCO)C1C=CC=CC=1\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eInChiKey:\u003c\/strong\u003e WQAGVQVBDHOHRD-UHFFFAOYSA-N\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eInChi:\u003c\/strong\u003e 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)\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eTechnical Data\u003c\/strong\u003e\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eAppearance:\u003c\/strong\u003e Solid Power\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003ePurity:\u003c\/strong\u003e ≥98% (or refer to the Certificate of Analysis)\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eShipping Condition:\u003c\/strong\u003e Shipped under ambient temperature as non-hazardous chemical or refer to Certificate of Analysis\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eStorage Condition:\u003c\/strong\u003e Dry, dark and -20 \u003csup\u003eo\u003c\/sup\u003eC for 1 year or refer to the Certificate of Analysis.\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eShelf Life:\u003c\/strong\u003e ≥12 months if stored properly.\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eStock Solution Storage:\u003c\/strong\u003e 0 - 4 \u003csup\u003eo\u003c\/sup\u003eC for 1 month or refer to the Certificate of Analysis.\u003c\/p\u003e\u003cp style=\"text-indent:-1em;padding-left:1em;\"\u003e\u003cstrong\u003eDrug Formulation:\u003c\/strong\u003e To be determined\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eHS Tariff Code:\u003c\/strong\u003e 382200\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eHow to use\u003c\/strong\u003e\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eIn Vitro:\u003c\/strong\u003e\u003c\/p\u003e\u003cp style=\"padding-left:1em;\"\u003eIn the profiling against a panel of 61 kinases, SR7826 (compound 18b) at 1 μM inhibits only Limk1 and STK16 with ≥80% inhibition. SR7826 is highly efficient in inhibiting cell-invasion\/migration in PC-3 cells. SR7826 (compound 18b) inhibits cofilin phosphorylation in A7r5 (IC50 = 470 nM) and PC-3 cells (IC50 \u0026lt; 1 µM). SR7826 (1 μM) inhibits contractions of prostate strips, which were induced by electrical field stimulation and inhibits cofilin phosphorylation in prostate tissues and cultured stromal cells (WPMY-1). In WPMY-1 cells, SR7826 causes breakdown of actin filaments and reduced viability.\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eIn Vivo:\u003c\/strong\u003e\u003c\/p\u003e\u003cp style=\"padding-left:1em;\"\u003eSR7826 (10 mg\/kg; oral gavage; once daily; for 11 days; hAPPJ20 mice) treatment significantly reduces the phosphorylation of cofilin at Ser3. SR7826 also increases both apical and basal thin spine density significantly in hAPPJ20 mice over mock-treated animals. The plasma pharmacokinetics studies on rats are investigated. After intravenous injection, the PK properties of SR7826 (compound 18b; 1mg\/kg) with a Cl of 5.2 mL\/min\/kg, a T1\/2 of 2.2h, an AUC of 8.4 μM*h and a Cmax of 7.7 μM, and has 36% oral bioavailability in rats (oral administration; 2mg\/kg).\u003c\/p\u003e\u003cp\u003e\u003cstrong\u003eProducts are for research use only. Not for human use.\u003c\/strong\u003e\u003c\/p\u003e","brand":"Xcess Biosciences","offers":[{"title":"M33148-C \/ Contact sales@xcessbio.com for quotation","offer_id":39551546032267,"sku":"0","price":100.0,"currency_code":"USD","in_stock":false}],"thumbnail_url":"\/\/cdn.shopify.com\/s\/files\/1\/0389\/1897\/9723\/products\/M33148_1636131550.gif?v=1636131552","url":"https:\/\/www.xcessbio.com\/products\/m33148","provider":"Xcess Biosciences","version":"1.0","type":"link"}