fluoro-Dapagliflozin [1181681-43-5]
Katalog-Nummer C5119-10mg
Size : 10mg
Marke : APExBIO Technology
Contact local distributor :
Telefonnummer : +1 850 650 7790
fluoro-Dapagliflozin
mRNA synthesis
In vitro transcription of capped mRNA with modified nucleotides and Poly(A) tail
Tyramide Signal Amplification (TSA)
TSA (Tyramide Signal Amplification), used for signal amplification of ISH, IHC and IC etc.
Phos Binding Reagent Acrylamide
Separation of phosphorylated and non-phosphorylated proteins without phospho-specific antibody
Cell Counting Kit-8 (CCK-8)
A convenient and sensitive way for cell proliferation assay and cytotoxicity assay
Inhibitor Cocktails
Protect the integrity of proteins from multiple proteases and phosphatases for different applications.
Ki: 5.3 and 330 nM for SGLT2 and SGLT1, respectively
fluoro-Dapagliflozin is a selective sodium-glucose cotransporter (SGLT) inhibitor.
Human Na(+)-D-glucose cotransporter (hSGLT) inhibitors constitute the newest class of diabetes drugs, blocking up to in-vivo 50% of renal glucose reabsorption.
In vitro: Dapagliflozin and fluoro-dapagliflozin could block glucose transport and glucose-coupled currents with around 100-fold specificity for hSGLT2 over hSGLT1. It was found that phlorizin and galacto-dapagliflozin rapidly dissociated from SGLT2, while fluoro-dapagliflozin dissociated from hSGLT2 at a rate 10-fold slower. In contrast, fluoro-dapagliflozin could quickly dissociate from hSGLT1 [1].
In vivo: Dapagliflozin, the close analog of fluoro-dapagliflozin, could acutely induce renal glucose excretion in normal and diabetic rats, improve glucose tolerance in normal rats, and reduce hyperglycemia in Zucker diabetic fatty at doses ranging from 0.1 to 1.0 mg/kg. Moreover, the once-daily dapagliflozin treatment was able to significantly lower fasting and fed glucose levels and led to a significant increase in glucose utilization rate [2].
Clinical trial: Clinical study found that dapagliflozin could lower hyperglycemia in treatment-naive patients with newly diagnosed type 2 diabetes, which made dapagliflozin a unique addition to existing treatment options for type 2 diabetes [3].
References:
[1] Hummel, C. S.,Lu, C.,Liu, J., et al. Structural selectivity of human SGLT inhibitors. American Journal of Physiology.Cell Physiology 302(2), C373-C382 (2012).
[2] Han, S. ,Hagan, D.L.,Taylor, J.R., et al. Dapagliflozin, a selective SGLT2 inhibitor, improves glucose homeostasis in normal and diabetic rats. Diabetes 57, 1723-1729 (2008).
[3] Ferrannini E, Ramos SJ, Salsali A, Tang W, List JF. Dapagliflozin monotherapy in type 2 diabetic patients with inadequate glycemic control by diet and exercise: a randomized, double-blind, placebo-controlled, phase 3 trial. Diabetes Care. 2010 Oct;33(10):2217-24.
- 1. Lin Y, Nan J, et al. "Canagliflozin impairs blood reperfusion of ischaemic lower limb partially by inhibiting the retention and paracrine function of bone marrow derived mesenchymal stem cells." EBioMedicine. 2020;52:102637. PMID:31981975
| Physical Appearance | A crystalline solid |
| Storage | Store at -20°C |
| M.Wt | 410.9 |
| Cas No. | 1181681-43-5 |
| Formula | C21H24ClFO5 |
| Synonyms | flouro-DAPA |
| Solubility | ≤30mg/ml in ethanol;30mg/ml in DMSO;30mg/ml in dimethyl formamide |
| Chemical Name | (1S)-1,5-anhydro-1-C-[4-chloro-3-[(4-ethoxyphenyl)methyl]phenyl]-4-deoxy-4-fluoro-D-glucitol |
| SDF | Download SDF |
| Canonical SMILES | ClC(C=CC([C@H]1[C@H](O)[C@@H](O)[C@H](F)[C@@H](CO)O1)=C2)=C2CC3=CC=C(OCC)C=C3 |
| Shipping Condition | Small Molecules with Blue Ice, Modified Nucleotides with Dry Ice. |
| General tips | We do not recommend long-term storage for the solution, please use it up soon. |
- Purity ≥ 95.00%
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COA (Certificate Of Analysis)
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