Turofexorate Isopropyl (XL335)
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 |
|---|---|---|
| 250mg | $1150 | Check With Us |
| 500mg | $1750 | Check With Us |
| 1g | $2625 | Check With Us |
: Cat #: V1842 CAS #: 629664-81-9 Purity ≥ 98%
Description: Turofexorate Isopropyl (also known as WAY-362450, Fxr 450 and XL335) is a novel, highly potent, selective and orally bioavailable FXR (farnesoid X receptor) agonist with EC50 of 4 nM, it is highly selective versus other nuclear receptors, such as LXR, PPAR, ER and etc.
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| Molecular Weight (MW) | 438.47 |
|---|---|
| Molecular Formula | C25H24F2N2O3 |
| CAS No. | 629664-81-9 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 33 mg/mL (75.3 mM)r |
| Water: <1 mg/mLr | |
| Ethanol: 2 mg/mL (4.6 mM) | |
| Solubility In Vivo | NMP+polyethylene glycol 300 (10+90, v+v): 30 mg/mL |
| SMILES Code | O=C(C1=CN(C(C2=CC=C(F)C(F)=C2)=O)CC(C)(C)C3=C1NC4=C3C=CC=C4)OC(C)C |
| Synonyms | Fxr 450; WAY-362450; WAY362450; WAY 362450; XL335; XL 335; XL-335; FXR-450; FXR 450; FXR450 |
| Protocol | In Vitro | Turofexorate isopropyl (WAY-362450) is a potent, selective, and orally bioavailable FXR agonist (EC50=4 nM). Turofexorate isopropyl (WAY-362450) is highly selective, as no significant cross-reactivity with these receptors (LXRα, LXRβ, PPARα, PPARγ, PPARδ, RXRα, RARγ, VDR, SXR, ERα, ERβ, GR, AR, MR, and PR) is observed at concentrations up to 10 μM. WAY-362450 displays potent agonist activity in the FXR reporter gene assays and on FXR target genes in cell-based assays. In promoter assays, utilizing reporter constructs under control of the human bile salt excretory pump (BSEP), human small heterodimer partner (SHP), and mouse intestinal bile acid binding protein (IBABP) genes are up-regulated by Turofexorate isopropyl (WAY-362450) with EC50 of 17, 230, and 33 nM, respectively. In addition, WAY-362450 significantly induces mRNAs encoding for BSEP, SHP, and IBABP in human cell cultures at 1 μM (13-, 2-, and 20-fold, respectively). |
|---|---|---|
| In Vivo | Turofexorate isopropyl (WAY-362450) also shows potent effects on cholesterol and triglyceride lowering in LDLR-/- mice and antiatherogenic activity with respect to reduction of aortic arch lesions. Oral administration of Turofexorate isopropyl (WAY-362450) to LDLR-/- mice results in lowering of cholesterol and triglycerides. Chronic administration in an atherosclerosis model results in significant reduction in aortic arch lesions. Turofexorate isopropyl (WAY-362450) is dosed in rat at 3 mg/kg (po and iv) and shows good oral bioavailability (38%). There is a protracted half-life of 25 h, modest volume of distribution, and low clearance (3.3 L/kg, ~10% of hepatic blood flow). Additional pharmacokinetic studies in mice and higher species have been completed, and the data will be reported elsewhere. |
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 | 2.2807 mL | 11.4033 mL | 22.8066 mL | 45.6132 mL |
| 5mM | 0.4561 mL | 2.2807 mL | 4.5613 mL | 9.1226 mL |
| 10mM | 0.2281 mL | 1.1403 mL | 2.2807 mL | 4.5613 mL |
| 20mM | 0.1140 mL | 0.5702 mL | 1.1403 mL | 2.2807 mL |
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Step One: Enter information below
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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.