Linagliptin
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 |
|---|---|---|
| 2g | $250 | Check With Us |
| 5g | $450 | Check With Us |
| 10g | $675 | Check With Us |
: Cat #: V0742 CAS #: 668270-12-0 Purity ≥ 98%
Description: Linagliptin (formerly known as BI-1356; trade names Tradjenta and Trajenta) is a xanthine-based, highly potent, selective, and competitive DPP-4 inhibitor with potential anti-diabetic activity.
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- Physicochemical and Storage Information
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- Related Biological Data
- Stock Solution Preparation
- Quality Control Documentation
| Molecular Weight (MW) | 472.54 |
|---|---|
| Molecular Formula | C25H28N8O2 |
| CAS No. | 668270-12-0 |
| Storage | -20℃ for 3 years in powder formr |
| -80℃ for 2 years in solvent | |
| Solubility In Vitro | DMSO: 17 mg/mL (36.0 mM)r |
| Water:<1 mg/mLr | |
| Ethanol: 1 mg/mL (2.1 mM) | |
| Solubility In Vivo | 0.5% hydroxyethyl cellulose: 30 mg/mL |
| SMILES Code | O=C(N1CC2=NC(C)=C3C=CC=CC3=N2)N(C)C4=C(N(CC#CC)C(N5C[C@H](N)CCC5)=N4)C1=O |
| Synonyms | Linagliptin; BI-1356; BI1356; BI 1356; trade names: Tradjenta, Trajenta |
| Protocol | In Vitro | Linagliptin inhibits DPP-4 activity in vitro in several independent experiments with IC50 values of 0.4, 0.5, 0.9, and 1.1 nM (mean IC50, approximately 1 nM). Linagliptin inhibits FAP with an IC50 of 89 nM (approximately 90-fold selectivity versus DPP-4). |
|---|---|---|
| In Vivo | In male Wistar rats, Beagle dogs, and Rhesus monkeys, xanthine linagliptin proves to be a highly efficacious, long-lasting, and potent DPP-4 inhibitor providing >70% inhibition for >7 h for all three species after oral administration of 1 mg/kg. Single oral administration of linagliptin to db/db mice 45 min prior to an oral glucose tolerance test reduced plasma glucose excursion in a dose-dependent manner from 0.1 mg/kg (15% inhibition) to 1 mg/kg (66% inhibition). |
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 | 2.1162 mL | 10.5811 mL | 21.1622 mL | 42.3245 mL |
| 5mM | 0.4232 mL | 2.1162 mL | 4.2324 mL | 8.4649 mL |
| 10mM | 0.2116 mL | 1.0581 mL | 2.1162 mL | 4.2324 mL |
| 20mM | 0.1058 mL | 0.5291 mL | 1.0581 mL | 2.1162 mL |
The molarity calculator equation
Mass(g) = Concentration(mol/L) × Volume(L) × Molecular Weight(g/mol)
Mass
=
Concentration
×
Volume
×
Molecular Weight*
The dilution calculator equation
Concentration(start)
×
Volume(start)
=
Concentration(final)
×
Volume(final)
This equation is commonly abbreviated as: C1 V1 = C2 V2
Concentration(start)
C1
×
Volume(start)
V1
=
Concentration(final)
C2
×
Volume(final)
V2
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.