Basic information Safety Supplier Related

K134

Basic information Safety Supplier Related

K134 Basic information

Product Name:
K134
Synonyms:
  • K134
  • 1-Cyclopropyl-1-((1R,2R)-2-hydroxycyclohexyl)-3-(3-((2-oxo-1,2-dihydroquinolin-6-yl)oxy)propyl)urea
  • OPC33509
  • Urea, N-cyclopropyl-N'-[3-[(1,2-dihydro-2-oxo-6-quinolinyl)oxy]propyl]-N-[(1R,2R)-2-hydroxycyclohexyl]-
  • K-134,K134
  • 1-cyclopropyl-1-[(1R,2R)-2-hydroxycyclohexyl]-3-[3-[(2-oxo-1H-quinolin-6-yl)oxy]propyl]urea
CAS:
189362-06-9
MF:
C22H29N3O4
MW:
399.48
Mol File:
189362-06-9.mol
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K134 Chemical Properties

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
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K134 Usage And Synthesis

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

K134Supplier

MedChemexpress LLC
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TargetMol Chemicals Inc.
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+1-781-999-5354; +17819995354
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Guangzhou Younan Technology Co., Ltd
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020-82000279 18988941452
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Beijing Jin Ming Biotechnology Co., Ltd.
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010-60605840 15801484223;
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psaitong@jm-bio.com
JinOu Biomedical (Nanjing) Co., Ltd.
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13000000000
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jinoupharma@163.com