RS-127445
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 |
|---|---|---|
| 500mg | $1200 | Check With Us |
| 1g | $1850 | Check With Us |
| 5g | $4990 | Check With Us |
: Cat #: V0968 CAS #: 199864-87-4 Purity ≥ 98%
Description: RS-127445 (RS 127445; RS127445) is a novel, potent, selective, and orally bioavailable 5-HT2B receptor antagonist with important biological activity.
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- Physicochemical and Storage Information
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- Related Biological Data
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| Molecular Weight (MW) | 281.33 |
|---|---|
| Molecular Formula | C17H16FN3 |
| CAS No. | 199864-87-4 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 56 mg/mL (199.1 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 8 mg/mL (28.4 mM) | |
| SMILES Code | CC(C1=CC(C2=C3C=CC=CC3=C(F)C=C2)=NC(N)=N1)C |
| Synonyms | MT500; RS-127445; RS 127445; RS127445; MT-500; MT 500. |
| Protocol | In Vitro | RS-127445 is found to has nanomolar affinity for the 5-HT2B receptor (pKi=9.5±0.1) and 1,000 fold selectivity for this receptor as compared to numerous other receptor and ion channel binding sites. RS-127445 potently displaces [3H]-5-HT from human recombinant 5-HT2B receptors expressed in CHO-K1 cells. The affinity (pKi value) of RS-127445 for the 5-HT2B receptor is 9.5±0.1 (n=9). RS-127445 is selective for the 5-HT2B receptor, having approximately 1000 fold lower affinity for the human recombinant 5-HT2C， 5-HT2A, 5-HT5, 5-HT6 and 5-HT7 receptors, a 5-HT1A receptor in rat brain membranes, a 5-HT1B/D receptor in bovine caudate, and a monoamine uptake site in rabbit platelets. RS-127445 potently blocks the 5-HT (10 nM) evoked increases in intracellular calcium concentrations in the HEK-293 cells expressing the 5-HT2B receptor (pIC50 of 10.4±0.1). In cells expressing human recombinant 5-HT2B receptors, RS-127445 potently antagonizes 5-HT-evoked formation of inositol phosphates (pKB=9.5±0.1) and 5-HT-evoked increases in intracellular calcium (pIC10=10.4±0.1). RS-127445 also blocks 5-HT-evoked contraction of rat isolated stomach fundus (pA2B=9.5±1.1) and (±)α-methyl-5-HT-mediated relaxation of the rat jugular vein (pA2=9.9±0.3) |
|---|
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 | 3.5545 mL | 17.7727 mL | 35.5454 mL | 71.0909 mL |
| 5mM | 0.7109 mL | 3.5545 mL | 7.1091 mL | 14.2182 mL |
| 10mM | 0.3555 mL | 1.7773 mL | 3.5545 mL | 7.1091 mL |
| 20mM | 0.1777 mL | 0.8886 mL | 1.7773 mL | 3.5545 mL |
The molarity calculator equation
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The dilution calculator equation
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Step One: Enter information below
Dosage mg/kg
Average weight of animals g
Dosing volume per animal µL
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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.