MK-4256 |
MK-4256 : Antagonist of SSTR3
Probe Summary
Selectivity
Potency
In Vivo
Control Compounds
Chemical Information
References
Vendors
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Probe Summary
| Targets | Biochemical/Biophysical Potency | Cellular Potency |
|---|---|---|
| SSTR3 |
|
Antagonist
100 nM
Selectivity
In Vitro Selectivity Assessment
Selectivity Assessment Description:
SSTR Subtype Selectivity of MK-4256 shows only SSTR3 as a target in both in vitro and functional ass ...
Potency Cellular
In Vitro
SSTR3
Mode of Action: Antagonist
Structure-Activity-Relationship data available? Yes
DOI Reference: 10.1021/ml300063m
In Vivo Validations
Mouse
Dose: 4 mg/Kg IV, 10 mg/Kg PO
Route of delivery:
Intravenous, Oral
Plasma half life:
1.52 h IV
Systemic clearance:
10.1 mL/min kg IV
Area Under the Curve::
19.3 μM*h PO
Bioavailability:
58% PO
Volume of Distribution at Steady-State:
1.66 L/Kg IV
Target engagement assay:
In a mouse oGTT assay MK-4256 reduces the glucose excursion from 0.003 to 10 mg/kg in a dose-dependent manner.
At 0.01, 0.1, and 1 mg/kg oral dose, MK-4256 achieved Cmax of 7, 88, and 493 nM, respectivley
DOI Reference: 10.1021/ml300063m
Rat
Dose: 1 mg/Kg IV, 2 mg/Kg PO
Route of delivery:
Intravenous, Oral
Plasma half life:
1.73 h IV
Systemic clearance:
34.0 mL/min*kg IV
Area Under the Curve::
0.81 μM*h PO
Bioavailability:
42% PO
Volume of Distribution at Steady-State:
5.1 L/kg IV
DOI Reference: 10.1021/ml300063m
Dog
Dose: 1 mg/Kg IV, 2 mg/Kg PO
Route of delivery:
Intravenous, Oral
Plasma half life:
7.0 h IV
Systemic clearance:
2.34 mL/min*kg IV
Area Under the Curve::
15.6 μM*h PO
Bioavailability:
53% PO
Volume of Distribution at Steady-State:
1.52 L/kg IV
DOI Reference: 10.1021/ml300063m
Monkey (Rheus)
Dose: 1 mg/Kg IV, 2 mg/Kg PO
Route of delivery:
Intravenous, Oral
Plasma half life:
7.21 h IV
Systemic clearance:
3.09 mL/min*kg IV
Area Under the Curve::
14.4 μM*h PO
Bioavailability:
65% PO
Volume of Distribution at Steady-State:
1.74 L/kg IV
DOI Reference: 10.1021/ml300063m
Chemical Information
| Molecular Formula | C27H23FN8O |
| SMILEs | Cc1nc([C@]2(c3cnn(C)c3)N[C@@H](c3nc(-c4ccc(F)cc4)c[nH]3)Cc3c2[nH]c2ccccc32)no1 |
| InChI | InChI=1S/C27H23FN8O/c1-15-31-26(35-37-15)27(17-12-30-36(2)14-17)24-20(19-5-3-4-6-21(19)32-24)11-22(34-27)25-29-13-23(33-25)16-7-9-18(28)10-8-16/h3-10,12-14,22,32,34H,11H2,1-2H3,(H,29,33)/t22-,27-/m1/s1 |
| Molecular weight | 494.20 Da |
| AlogP | 4.30092 |
| HBond acceptors | 9 |
| HBond donors | 3 |
| Atoms | 60 |
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