MK-4256
This product is for research use only, not for human use. We do not sell to patients.
For small sizes, please check our retail website as below: www.invivochem.com
| Size | Price | Stock |
|---|---|---|
| 50mg | $1850 | Check With Us |
| 100mg | $3150 | Check With Us |
| 200mg | $4725 | Check With Us |
: Cat #: V4290 CAS #: 1104599-69-0 Purity ≥ 98%
Description: MK-4256 is a novel, potent and selective SSTR3 (somatostatin subtype receptor 3) antagonist with IC50s of 0.66 nM and 0.36 nM in human and mouse receptor binding assays, respectively.
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| Molecular Weight (MW) | 494.52 |
|---|---|
| Molecular Formula | C27H23FN8O |
| CAS No. | 1104599-69-0 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent |
| Protocol | In Vitro | MK-4256 has excellent selectivity against other SSTR subtypes based on in vitro assays. In human receptor binding assays, MK-4256 has IC50s >2 μM for SSTR1 and SSTR2. Although the binding IC50 values on SSTR4 and SSTR5 are below 1 μM, there is still >500-fold selectivity. MK-4256 is tested in functional antagonist assays against SSTR4 and SSTR5. The IC50 values are greater than 5 μM (at least 5000-fold selectivity) |
|---|---|---|
| In Vivo | MK-4256 reduces glucose excursion in a dose-dependent fashion with maximal efficacy achieves at doses as low as 0.03 mg/kg po. MK-4256 demonstrates exceptional SSTR3-mediated glucose-lowering efficacy in the mouse oGTT model with minimal hypoglycemia risk. MK-4256 achieves complete ablation of glucose excursion (109%) at 1 mg/kg po. MK-4256 reduces the glucose excursion from 0.003 to 10 mg/kg in a dose-dependent manner. The plasma Cmax of MK-4256 is determined from parallel mouse PK studies. At 0.01, 0.1, and 1 mg/kg oral dose, MK-4256 achieves Cmax of 7, 88, and 493 nM, respectivley |
These protocols are for reference only. InvivoChem does not
independently validate these methods.
| Solvent volume to be added | Mass (the weight of a compound) | |||
|---|---|---|---|---|
| Mother liquor concentration | 1mg | 5mg | 10mg | 20mg |
| 1mM | 2.0222 mL | 10.1108 mL | 20.2216 mL | 40.4433 mL |
| 5mM | 0.4044 mL | 2.0222 mL | 4.0443 mL | 8.0887 mL |
| 10mM | 0.2022 mL | 1.0111 mL | 2.0222 mL | 4.0443 mL |
| 20mM | 0.1011 mL | 0.5055 mL | 1.0111 mL | 2.0222 mL |
The molarity calculator equation
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Molecular Weight*
The dilution calculator equation
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This equation is commonly abbreviated as: C1 V1 = C2 V2
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Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
Number of animals
Step Two: Enter the in vivo formulation
%DMSO
+
%
+
%Tween 80
+
%ddH2O
Calculation Results:
Working concentration:
mg/ml;
Method for preparing DMSO master liquid:
mg
drug pre-dissolved in
µL
DMSO(Master liquid concentration
mg/mL)
,Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.
Method for preparing in vivo formulation:
Take
µL
DMSO master liquid, next add
µL
PEG300, mix and clarify, next add
µL
Tween 80,mix and clarify, next add
µL
ddH2O,mix and clarify.
Note:
- (1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
- (2) Be sure to add the solvent(s) in order.