trans-4-[(r)-1-aminoethyl]-n-(4-pyridyl)cyclohexanecarboxamide dihydrochloride y 27632 dihydrochloride (2024)

Y-27632 dihydrochloride

CAS: 129830-38-2

Molecular Formula: C14H23Cl2N3O

trans-4-[(r)-1-aminoethyl]-n-(4-pyridyl)cyclohexanecarboxamide dihydrochloride y 27632 dihydrochloride - Names and Identifiers

Name	Y-27632 dihydrochloride
Synonyms	Y-27632 CS-1919 Y27632 Y 27632 ROCK INHIBITOR Y27632 (HYDROCHLORIDE) Y27632 DIHYDROCHLORIDE Y27632 (hydrochloride) Y-27632 DIHYDROCHLORIDE Y-27632 dihydrochloride Y 27632 DIHYDROCHLORIDE RHO-KINASE INHIBITOR Y-27632 (R)-4-(1-aminoethyl)-N-(pyridin-4-yl)cyclohexanecarboxamide dihydrochloride trans-4-[(R)-1-Aminoethyl]-N-(4-pyridyl)cyclohexanecarboxamide dihydrochloride trans-4-[(R)-1-Aminoethyl]-N-(4-pyridyl)cyclohexanecarboxamide dihydrochloride Y 27632 dihydrochloride
CAS	129830-38-2
EINECS	813-428-5

trans-4-[(r)-1-aminoethyl]-n-(4-pyridyl)cyclohexanecarboxamide dihydrochloride y 27632 dihydrochloride - Physico-chemical Properties

Molecular Formula	C14H23Cl2N3O
Molar Mass	320.25792
Melting Point	258℃
Solubility	DMSO:64 mg/mL warmed (199.83 mM);Water:14 mg/mL (43.71 mM);Ethanol Insoluble
Appearance	Morphological powder
Color	white to beige
Storage Condition	2-8°C
Stability	Stable for 2 years from date of purchase as supplied. Solutions in DMSO or methanol may be stored at -20° for up to 3 months.
MDL	MFCD03490488
Physical and Chemical Properties	Bioactive Y-27632 2HCl is a selective ROCK1(p160ROCK) inhibitor. Ki is 140 nM in cell-free test, which is more than 200 times stronger than other kinases including PKC,cAMP-dependent protein kinase, MLCK and PAK.
Use	Product Description Y-27632 2HCl is a selective ROCK1(p160ROCK) inhibitor, Ki is 140 nM, which is more than 200 times more selective than acting on other kinases, including PKC,cAMP-dependent protein kinase, MLCK and PAK. The target ROCK1 ROCK2IC50140 nM (Ki) 300 nM (Ki)In VitroY-27632 is equally effective in inhibiting ROCK-II. Y-27632 acting on PKC, cAMP-dependent protein kinase, and myosin light chain kinase (MLCK) had little activity with Ki of 26 μM, 25 μM, and> amp; gt; 250 μM, respectively. Y-27632 inhibit various stimulants instead of KCl, including Phenylephrine, Histamine, Acetylcholine, Serotonin, Endothelin, and Thromboxane-induced smooth muscle contraction by selectively inhibiting Ca2 + sensitization, IC50 is 0.3-1 μM. Y-27632 acts on cultured cells to inhibit Rho-induced, p160ROCK-regulated stress fiber formation. Y-27632 treatment blocks the activation of Rho-regulated actomyosin and also blocks the invasion activity of MM1 cells stimulated by LPA, which is concentration-dependent. Human embryonic stem cells (hES) treated with 10 μM Y-27632 in serum-free suspension (SFEB) medium significantly reduced separation-induced apoptosis, improved cloning efficiency (from ~ 1% to ~ 27%), promoted subcloning after transgene, and allowed SFEB cultured hES cells to survive and differentiate into Bf1 + cortical and basal progenitor cells. In VivoY-27632 treated spontaneously hypertensive rats, renal hypertensive rats and deoxycorticosterone acetic acid (DOCA) salt hypertensive rats orally at a dose of 30 mg/kg significantly reduced blood pressure, which was dose-dependent. Y-27632 rats expressing Val14-RhoA were continuously treated by implantation pump at 0.55 μL per hour for 11 days, delaying MM1 cell invasion. Y-27632 acts on the pulmonary circulation to reduce hypoxia-induced angiogenesis and vascular remodeling by inhibiting ROCK.
In vitro study	Y-27632 is equally effective in inhibiting ROCK-II. Y-27632 had little activity on PKC, cAMP-dependent protein kinase, and myosin light chain kinase (MLCK), with K I of 26 μm, 25 μm, and> 250 μm, respectively. Y-27632 blocking Rho-regulated actomyosin activation by selective inhibition of Ca Y-27632 treatment also blocks LPA-stimulated MM1 cell invasion activity in a concentration-dependent manner. 10 μm Y-27632 treatment of human embryonic stem cells (hES) in serum-free suspension (SFEB) media significantly reduced isolation-induced apoptosis, cloning efficiency was increased (from -1% to-27%), subcloning was promoted after transgene, and SFEB-cultured hES cells survived and differentiated into Bf1 + cortical and basal telencephalon progenitor cells.
In vivo study	Y-27632 according to the dose of 30 mg/kg oral treatment of spontaneously hypertensive rats, renal hypertensive rats, and deoxycorticosterone acetate (DOCA) salt hypertensive rats, significantly reduced blood pressure, this effect is dose dependent. Y-27632 expression Val was treated continuously at 0.55 μl/hr by implanted pump Y-27632 acts on the pulmonary circulation, reduces hypoxia-induced angiogenesis, and vascular remodeling by inhibiting ROCK.

trans-4-[(r)-1-aminoethyl]-n-(4-pyridyl)cyclohexanecarboxamide dihydrochloride y 27632 dihydrochloride - Risk and Safety

Hazard Symbols	Xn - Harmful
Risk Codes	20/21/22 - Harmful by inhalation, in contact with skin and if swallowed.
Safety Description	36 - Wear suitable protective clothing.
WGK Germany	3
HS Code	29333990

trans-4-[(r)-1-aminoethyl]-n-(4-pyridyl)cyclohexanecarboxamide dihydrochloride y 27632 dihydrochloride - Preparation solution concentration reference

	1mg	5mg	10mg
1 mM	3.122 ml	15.612 ml	31.225 ml
5 mM	0.624 ml	3.122 ml	6.245 ml
10 mM	0.312 ml	1.561 ml	3.122 ml
5 mM	0.062 ml	0.312 ml	0.624 ml

Last Update：2024-01-02 23:10:35

trans-4-[(r)-1-aminoethyl]-n-(4-pyridyl)cyclohexanecarboxamide dihydrochloride y 27632 dihydrochloride - Reference Information

biological activity	Y-27632 2HCl is a selective ROCK1(p160ROCK) inhibitor. Ki is 140 nM in cell-free test, which is more than 200 times stronger than other kinases including PKC,cAMP-dependent protein kinase, MLCK and PAK.
target	TargetValue ROCK1 (p160ROCK) (cell-free assessment) 140 nM (ki) ROCK2 (cell-free assessment) 300 nM (ki)
Target	Value
ROCK1 (p160ROCK)(Cell-free assay)	140 nM(Ki)
ROCK2(Cell-free assay)	300 nM(Ki)
in vitro studies	Y-27632 are equally effective in inhibiting ROCK-II. Y-27632 acting on PKC, cAMP-dependent protein kinase, and myosin light chain kinase (MLCK) had little activity, with K I being 26 μM, 25 μM, and> amp; gt; 250 μM, respectively. Y-27632 block the activation of Rho-regulated actomyosin and LPA-stimulated MM1 cell invasion activity by selectively inhibiting Ca Y-27632 treatment, which is concentration-dependent. Human embryonic stem cells (hES) treated with 10 μM Y-27632 in serum-free suspension (SFEB) medium significantly reduced separation-induced apoptosis, improved cloning efficiency (from ~ 1% to ~ 27%), promoted subcloning after transgene, and allowed SFEB cultured hES cells to survive and differentiate into Bf1 + cortical and basal progenitor cells.
in vivo study	Y-27632 orally treated spontaneously hypertensive rats, renal hypertensive rats and deoxycorticosterone acetic acid (DOCA) salt hypertensive rats at a dose of 30 mg/kg, significantly reducing blood pressure, which is dose-dependent. Y-27632 0.55 μL per hour, Val Y-27632 is continuously treated by implantation pump to act on pulmonary circulation, and hypoxia-induced angiogenesis and vascular remodeling are reduced by inhibiting ROCK.

Last Update：2024-04-10 22:29:15

trans-4-[(r)-1-aminoethyl]-n-(4-pyridyl)cyclohexanecarboxamide dihydrochloride y 27632 dihydrochloride - Uses and synthesis methods

Target

Target Value

ROCK1 (p160ROCK)

(Cell-free assay) 140 nM(Ki)

ROCK2

(Cell-free assay) 300 nM(Ki)

in vitro studies

Y-27632 is equally effective in inhibiting ROCK-II. Y-27632 acting on PKC, cAMP-dependent protein kinase, and myosin light chain kinase (MLCK) had little activity, with K I being 26 μM, 25 μM, and> amp; gt; 250 μM, respectively. Y-27632 block the activation of Rho-regulated actomyosin and LPA-stimulated MM1 cell invasion activity by selectively inhibiting Ca Y-27632 treatment, which is concentration-dependent. Human embryonic stem cells (hES) treated with 10 μM Y-27632 in serum-free suspension (SFEB) medium significantly reduced separation-induced apoptosis, improved cloning efficiency (from ~ 1% to ~ 27%), promoted subcloning after transgene, and allowed SFEB cultured hES cells to survive and differentiate into Bf1 + cortical and basal progenitor cells.

In vivo studies

Y-27632 orally treated spontaneously hypertensive rats, renal hypertensive rats, and deoxycorticosterone acetic acid (DOCA) salt hypertensive rats at a dose of 30 mg/kg significantly reduced blood pressure, which was dose-dependent. Y-27632 0.55 μL per hour, Val Y-27632 is continuously treated by implantation pump to act on pulmonary circulation, and hypoxia-induced angiogenesis and vascular remodeling are reduced by inhibiting ROCK.

Last Update：2024-04-10 22:29:15

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