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Cofrogliptin

Cat No.:V44361 Purity: ≥98%
Cofrogliptin (HSK7653) (compound 2), a tetrahydropyran analogue, is a potent oral DPP-4 inhibitor (antagonist) with long-lasting hypoglycemic effects.
Cofrogliptin
Cofrogliptin Chemical Structure CAS No.: 1844874-26-5
Product category: New3
This product is for research use only, not for human use. We do not sell to patients.
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Product Description
Cofrogliptin (HSK7653) (compound 2), a tetrahydropyran analogue, is a potent oral DPP-4 inhibitor (antagonist) with long-lasting hypoglycemic effects. Cofrogliptin (compound 2) has great potential in type 2 diabetes (T2DM) applications.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
Cofrogliptin (HSK7653) (compound 2) exhibits DPP-4 inhibitory action, with an IC50 of 4.18 nM[2].
ln Vivo
Cofrogliptin (HSK7653) (Compound 2) (IV: 0.5 mg/kg; PO: 2 mg/kg) demonstrates an unusually long half-life and a modest rate of reduction in drug concentration after oral administration. Colagliptin (Compound 2) (single dosage, oral, 3 mg/kg, 10 mg/kg, 30 mg/kg) has prolonged half-life, high oral exposure, venous clearance and hepatic microsomal clearance after intravenous injection Low. Cofrogliptin (Compound 2) (single dose, oral, 10 mg/kg) displayed extended DPP-4 inhibition in ob/ob mice and lowered HbA1c levels at dosages of 3 and 10 mg/kg. Cofrogliptin (compound 2) (single dose, oral, 10 mg/kg) also has significant potential for biweekly treatment of T2DM in rhesus monkeys [2]. ICR mouse pharmacokinetic parameters [2] IV (dose: 0.5 mg/kg) PO (dose: 2 mg/kg) CI (mL/min/kg) Vdss (L/kg) t1/2 (h) Cmax (ng/ mL) t1/2(h) AUC0-t(ng·h/mL) F% Ologliptin 7.39±2.1 1.65±0.27 3.05±0.6 798±122 4.65±1.4 4095±552 95.0±29 Kaog Gliptin (compound 2) 2.57±0.09 3.30±0.33 25.6±9.6 352±20 29.9±3.2 7898±873 62.2±6.9
Animal Protocol
Animal/Disease Models: ob/ob mice[2]
Doses: 3 mg/kg, 10 mg/kg, 30 mg/kg.
Route of Administration: single dose, oral administration, 3 mg/kg, 10 mg/kg, 30 mg/kg.
Experimental Results: It demonstrated strong inhibitory ability on plasma DPP-4 in a dose-dependent manner.

Animal/Disease Models: Rhesus monkey[2]
Doses: 10 mg/kg
Route of Administration: Single oral administration, 10 mg/kg
Experimental Results:It has more than 80% plasma DPP-4 inhibition ability, which lasts for at least 12 days. The plasma DPP-4 inhibition rates at the second and third weeks after administration were 76.16% and 43.41% respectively.
References

[1]. International Nonproprietary Names for Pharmaceutical Substances (INN).

[2]. Design, Synthesis, and Evaluation of a Series of Novel Super Long-Acting DPP-4 Inhibitors for the Treatment of Type 2 Diabetes. J Med Chem. 2020 Jul 9;63(13):7108-7126.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C18H19F5N4O3S
Molecular Weight
466.43
Exact Mass
466.109
CAS #
1844874-26-5
PubChem CID
118613788
Appearance
White to off-white solid powder
LogP
1.4
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
11
Rotatable Bond Count
3
Heavy Atom Count
31
Complexity
766
Defined Atom Stereocenter Count
4
SMILES
C([C@@H]1[C@@H](C[C@@H]([C@H](O1)C1C=C(C=CC=1F)F)N)N1CC2C(C1)=NN(S(=O)(C)=O)C=2)(F)(F)F
InChi Key
GUBOXFWNNXSQNH-SVGFKBNWSA-N
InChi Code
InChI=1S/C18H19F5N4O3S/c1-31(28,29)27-7-9-6-26(8-14(9)25-27)15-5-13(24)16(30-17(15)18(21,22)23)11-4-10(19)2-3-12(11)20/h2-4,7,13,15-17H,5-6,8,24H2,1H3/t13-,15+,16+,17-/m0/s1
Chemical Name
(2R,3S,5R,6S)-2-(2,5-difluorophenyl)-5-(2-methylsulfonyl-4,6-dihydropyrrolo[3,4-c]pyrazol-5-yl)-6-(trifluoromethyl)oxan-3-amine
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~100 mg/mL (~214.39 mM)
Solubility (In Vivo)
Solubility in Formulation 1: ≥ 1.25 mg/mL (2.68 mM) (saturation unknown) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

Solubility in Formulation 2: ≥ 1.25 mg/mL (2.68 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 12.5 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.

 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 2.1439 mL 10.7197 mL 21.4394 mL
5 mM 0.4288 mL 2.1439 mL 4.2879 mL
10 mM 0.2144 mL 1.0720 mL 2.1439 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

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Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution 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 stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(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.

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