K134
- Product Name
- K134
- CAS No.
- 189362-06-9
- Chemical Name
- K134
- Synonyms
- K134;OPC33509;K-134,K134;1-cyclopropyl-1-[(1R,2R)-2-hydroxycyclohexyl]-3-[3-[(2-oxo-1H-quinolin-6-yl)oxy]propyl]urea;1-Cyclopropyl-1-((1R,2R)-2-hydroxycyclohexyl)-3-(3-((2-oxo-1,2-dihydroquinolin-6-yl)oxy)propyl)urea;Urea, N-cyclopropyl-N'-[3-[(1,2-dihydro-2-oxo-6-quinolinyl)oxy]propyl]-N-[(1R,2R)-2-hydroxycyclohexyl]-
- CBNumber
- CB93339663
- Molecular Formula
- C22H29N3O4
- Formula Weight
- 399.48
- MOL File
- 189362-06-9.mol
K134 Property
- Boiling point:
- 731.4±60.0 °C(Predicted)
- Density
- 1.29±0.1 g/cm3(Predicted)
- storage temp.
- 4°C, away from moisture and light
- solubility
- Soluble in DMSO
- form
- Solid
- pka
- 11.13±0.70(Predicted)
- color
- White to off-white
K134 Chemical Properties,Usage,Production
Uses
K134 is a phosphodiesterase 3 (PDE3) inhibitor. The IC50s of K134 toward PDE3A, PDE3B, PDE5, PDE2 and PDE4 are 0.1, 0.28, 12.1, >300 and >300 μM, respectively.
in vivo
K134 (K-134) significantly prolongs middle cerebral artery (MCA) occlusion time at doses >10 mg/kg, and reduces cerebral infarct size at 30 mg/kg in the stroke model (n?=?12, 87.5±5.6 vs. 126.8±7.5 mm3, P<0.01), indicating its potent antithrombotic effect. The overall bleeding risk of K134 is assessed in general in mice. Single oral administration of K134 does not prolong bleeding time at a dose of 30 mg/kg compared to control (106±5 vs. 110±5 s, not significant). Moreover, a sufficiently high enough plasma concentration of K134 (13.6±2.3 μM) is detected to inhibit platelet aggregation at 10 min after single administration in mice at a dose of 30 mg/kg, which is the same time point as the above test of bleeding time. Next, the effects of PDE3 inhibitors on thrombus formation are also investigated in an arteriovenous shunt model in rats. K134 significantly reduces the incidence of occlusive shunt thrombi at doses above 10 mg/kg (half-maximal effective dose: ED50=11 mg/kg). The plasma concentration of K134 is 0.43±0.08 μM (Cmax) at a dose of 10 mg/kg[1].
IC 50
PDE2; PDE3
References
[1] Yoshida H, et al. K-134, a phosphodiesterase 3 inhibitor, prevents brain damage by inhibiting thrombus formation in a rat cerebral infarction model. PLoS One. 2012;7(10):e46432. DOI:10.1371/journal.pone.0046432
K134 Preparation Products And Raw materials
Raw materials
Preparation Products
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View Lastest Price from K134 manufacturers
- Product
- 1-cyclopropyl-1-[(1R,2R)-2-hydroxycyclohexyl]-3-[3-[(2-oxo-1H-quinolin-6-yl)oxy]propyl]urea 189362-06-9
- Price
- US $2.00-5.00/kg
- Min. Order
- 1kg
- Purity
- 99%
- Supply Ability
- 100kg
- Release date
- 2025-06-23