- Cart - 0 item(s)
- $0.00
Your shopping cart is empty!
- Chemistry
- Bioactive Molecules
- Anti-infection
- Apoptosis
- Autophagy
- Cell Cycle/DNA Damage
- Cytoskeleton
- Epigenetics
- GPCR/G Protein
- Immunology/Inflammation
- JAK/STAT Signaling
- MAPK/ERK Pathway
- Membrane Transporter/Ion Channel
- Metabolic Enzyme/Protease
- Neuronal Signaling
- NF-κB
- PI3K/Akt/mTOR
- PROTAC
- Protein Tyrosine Kinase/RTK
- Stem Cell/Wnt
- TGF-beta/Smad
- Vitamin D Related/Nuclear Receptor
- Others
- Methylation
- Cytoskeletal Signaling
- Natural Products
- Alkaloids
- Amino acid
- Anthraquinones
- Cerebrosides
- Chalcones
- Coumarins
- Diterpenoids
- Flavonoids
- Iridoids
- Lignans
- Lipids
- Miscellaneous
- Monoterpenoids
- Other terpenes
- Phenols
- Phenylpropanoids
- Quinones
- Saccharides
- Sesquiterpenoids
- Steroids
- Tetraterpenoids
- Thiophenes
- Triterpenoids
- Xanthones
- Polyphenols
- Stibene glucosides
- Oligose
- Anthocyanins
- Miscellaneous
- Chromones
- Terpenoids
- Indoles
- Procyanidins
- Aliphatics
- Botanical Cyclopeptides
- ADCs
- Antibodies
- Multiplex IHC
- Material Science
- Others
[CAS NO. 1210344-83-4] ErtugliflozinL-pyroglutamicacid
| Ships within | Stock | Price | Qty | Total |
Please click "REQUEST A QUOTE" button if there is no stock, or you need other sizes or custom synthesis.
| Catalog: | HY-15461A |
| Brand: | MCE |
| CAS: | 1210344-83-4 |
Overview
| MDL | - |
|---|---|
| Molecular Weight | 566.00 |
| Molecular Formula | C27H32ClNO10 |
| SMILES | ClC1=CC=C([C@]23O[C@@](CO)(CO3)[C@@H](O)[C@H](O)[C@H]2O)C=C1CC4=CC=C(OCC)C=C4.O=C5CC[C@@H](C(O)=O)N5 |
1 Publications Citing Use of MCE
Summary
IC50 & Target
IC50: 0.877 nM (h-SGLT2) [1] .
In Vitro
Ertugliflozin L-pyroglutamic acid (PF-04971729 L-pyroglutamic acid) demonstrates >2000-fold selectivity for SGLT2 inhibition (relative to SGLT1) in vitro [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
In Vivo
Ertugliflozin L-pyroglutamic acid (PF-04971729 L-pyroglutamic acid) reveals a concentration-dependent glucosuria after oral administration to rats [3] .
MCE has not independently confirmed the accuracy of these methods. They are for reference only.
Clinical Trial
| NCT Number | Sponsor | Condition | Start Date | Phase |
|---|---|---|---|---|
| NCT02226003 | Merck Sharp & Dohme LLC|Pfizer |
Type 2 Diabetes Mellitus
|
September 23, 2014 | Phase 3 |
| NCT04438213 | Yale University|Merck Sharp & Dohme LLC |
Heart Failure
|
March 10, 2021 | Phase 2 |
| NCT02033889 | Merck Sharp & Dohme LLC|Pfizer |
Type 2 Diabetes Mellitus
|
December 13, 2013 | Phase 3 |
| NCT01054300 | Merck Sharp & Dohme LLC|Pfizer |
Diabetes Mellitus, Type 2|Adult
|
February 17, 2010 | Phase 1 |
| NCT04167761 | Stanford University|Merck Sharp & Dohme LLC |
Cardiovascular Diseases|Atherosclerosis|Type 2 Diabetes|Insulin Resistance
|
July 1, 2020 | Early Phase 1 |
| NCT01999218 | Merck Sharp & Dohme LLC|Pfizer |
Type 2 Diabetes Mellitus
|
December 16, 2013 | Phase 3 |
| NCT04071626 | University Hospitals Cleveland Medical Center |
Heart Failure, Diastolic|Diabetes Mellitus, Type 2
|
March 1, 2020 | Phase 4 |
| NCT01096667 | Merck Sharp & Dohme LLC|Pfizer |
Diabetes Mellitus, Type 2|Hypertension
|
May 17, 2010 | Phase 2 |
| NCT02411929 | Merck Sharp & Dohme LLC|Pfizer |
Type 2 Diabetes Mellitus
|
October 29, 2014 | Phase 1 |
| NCT01986855 | Merck Sharp & Dohme LLC|Pfizer |
Type 2 Diabetes Mellitus
|
December 2, 2013 | Phase 3 |
| NCT01018823 | Merck Sharp & Dohme LLC|Pfizer |
Healthy Volunteer
|
December 14, 2009 | Phase 1 |
| NCT01059825 | Merck Sharp & Dohme LLC|Pfizer |
Diabetes Mellitus, Type 2
|
February 24, 2010 | Phase 2 |
| NCT05612594 | Yale University|Case Western Reserve University |
Sleep Apnea
|
November 2022 | Phase 4 |
| NCT04490681 | Yonsei University |
Heart Failure With Nonischemic Cardiomyopathy
|
August 2020 | Phase 3 |
| NCT02115347 | Merck Sharp & Dohme LLC|Pfizer |
Type 2 Diabetes Mellitus|Hepatic Impairment
|
September 19, 2014 | Phase 1 |
| NCT04231331 | Asan Medical Center|Merck Sharp & Dohme LLC |
Mitral Valve Insufficiency|Left Ventricular Systolic Dysfunction
|
November 4, 2020 | Phase 3 |
| NCT04027530 | Amsterdam UMC, location VUmc |
Type 2 Diabetes Mellitus|Diabetic Kidney Disease|Diabetic Nephropathy|Renal Hypoxia|Renoprotection|SGLT2 Inhibitor|Ertugliflozin
|
December 10, 2020 | Phase 4 |
| NCT01986881 | Merck Sharp & Dohme LLC|Pfizer |
Type 2 Diabetes Mellitus
|
November 4, 2013 | Phase 3 |
| NCT03416270 | University Health Network, Toronto|University Medical Center Groningen|Merck Sharp & Dohme LLC|University of Toronto|Toronto General Hospital |
Type 2 Diabetes Mellitus|Heart Failure
|
May 7, 2018 | Phase 2 |
| NCT05152940 | Icahn School of Medicine at Mount Sinai |
Heart Failure With Reduced Ejection Fraction|Congestion
|
November 2022 | Phase 4 |
| NCT01948986 | Merck Sharp & Dohme LLC|Pfizer |
Renal Impairment|Type 2 Diabetes Mellitus
|
October 1, 2013 | Phase 1 |
| NCT01127308 | Merck Sharp & Dohme LLC|Pfizer |
Type 2 Diabetes Mellitus (T2DM)
|
June 2010 | Phase 1 |
| NCT03640221 | Cedars-Sinai Medical Center|Merck Sharp & Dohme LLC |
Hypertension|Diabetes Mellitus, Type 2
|
September 1, 2018 | Phase 4 |
| NCT02036515 | Merck Sharp & Dohme LLC|Pfizer |
Type 2 Diabetes Mellitus
|
March 12, 2014 | Phase 3 |
| NCT01114568 | Merck Sharp & Dohme LLC|Pfizer |
Healthy
|
May 2010 | Phase 1 |
| NCT02630706 | Merck Sharp & Dohme LLC|Pfizer |
Type 2 Diabetes Mellitus
|
December 16, 2015 | Phase 3 |
| NCT03717194 | Soo Lim|MSD Korea Ltd.|Seoul National University Bundang Hospital |
Type2 Diabetes|Heart Failure
|
June 1, 2019 | Phase 3 |
| NCT00989079 | Merck Sharp & Dohme LLC|Pfizer |
Type 2 Diabetes Mellitus
|
October 16, 2009 | Phase 1 |
| NCT02099110 | Merck Sharp & Dohme LLC|Pfizer |
Type 2 Diabetes Mellitus
|
April 22, 2014 | Phase 3 |
| NCT01958671 | Merck Sharp & Dohme LLC|Pfizer |
Type 2 Diabetes Mellitus
|
October 9, 2013 | Phase 3 |
| NCT04029480 | Merck Sharp & Dohme LLC|Pfizer |
Type 2 Diabetes Mellitus
|
October 8, 2019 | Phase 3 |
| NCT01223339 | Merck Sharp & Dohme LLC|Pfizer |
Diabetes Mellitus, Type 2
|
October 2010 | Phase 1 |
| NCT04600921 | Medical University of Graz|Klinikum Klagenfurt am Wörthersee|Elisabethinen Hospital|Klinik Ottakring|Medical University Innsbruck|Medical University of Vienna|General Hospital Linz|Landesklinkum Wiener Neustadt |
Heart Failure With Reduced Ejection Fraction|Heart Failure With Mid Range Ejection Fraction|Implantable Cardioverter-Defibrillators|Cardiac Resynchronization Therapy
|
June 24, 2021 | Phase 3 |
Appearance
Solid
Shipping
Room temperature in continental US; may vary elsewhere.
Storage
| Powder | -20°C | 3 years |
|---|---|---|
| 4°C | 2 years | |
| In solvent | -80°C | 6 months |
| -20°C | 1 month |
Solvent & Solubility
DMSO : ≥ 125 mg/mL ( 220.85 mM )
H 2 O : 5 mg/mL ( 8.83 mM ; ultrasonic and warming and heat to 60°C)
* "≥" means soluble, but saturation unknown.
Stock Solutions
| Concentration Solvent Mass | 1 mg | 5 mg | 10 mg |
|---|
| 1 mM | 1.7668 mL | 8.8339 mL | 17.6678 mL |
| 5 mM | 0.3534 mL | 1.7668 mL | 3.5336 mL |
| 10 mM | 0.1767 mL | 0.8834 mL | 1.7668 mL |
References
- [1] Mascitti V, et al. Discovery of a clinical candidate from the structurally unique dioxa-bicyclo[3.2.1]octane class of sodium-dependent glucose cotransporter 2 inhibitors. J Med Chem. 2011 Apr 28;54(8):2952-60.
- [2] Miao Z, et al. Pharmacokinetics, metabolism, and excretion of the antidiabetic agent ertugliflozin (PF-04971729) in healthy male subjects. Drug Metab Dispos. 2013 Feb;41(2):445-56.
- [3] Kalgutkar AS, et al. Preclinical species and human disposition of PF-04971729, a selective inhibitor of the sodium-dependent glucose cotransporter 2 and clinical candidate for the treatment of type 2 diabetes mellitus. Drug Metab Dispos. 2011 Sep;39(9):16
Arctom is a premier supply platform offering over 600K unique items of Building Blocks, Bioactive Molecules, Natural Products, ADC PEG Linkers, Antibodies, and other Research Chemicals for global pharmaceutical, biotech, university, and industrial customers. We accelerate your research by providing better and faster purchasing experience & services.