Synonym
CX08005; CX-08005; CX 08005;
IUPAC/Chemical Name
N-(2-Tetradecyloxy-phenyl)-phthalamic acid
InChi Key
WOEDXTWDPRNPMZ-UHFFFAOYSA-N
InChi Code
InChI=1S/C28H39NO4/c1-2-3-4-5-6-7-8-9-10-11-12-17-22-33-26-21-16-15-20-25(26)29-27(30)23-18-13-14-19-24(23)28(31)32/h13-16,18-21H,2-12,17,22H2,1H3,(H,29,30)(H,31,32)
SMILES Code
O=C(O)C1=CC=CC=C1C(NC2=CC=CC=C2OCCCCCCCCCCCCCC)=O
Purity
>98% (or refer to the Certificate of Analysis)
Shipping Condition
Shipped under ambient temperature as non-hazardous chemical. This product is stable enough for a few weeks during ordinary shipping and time spent in Customs.
Storage Condition
Dry, dark and at 0 - 4 C for short term (days to weeks) or -20 C for long term (months to years).
Solubility
Soluble in DMSO
Shelf Life
>3 years if stored properly
Drug Formulation
This drug may be formulated in DMSO
Stock Solution Storage
0 - 4 C for short term (days to weeks), or -20 C for long term (months).
HS Tariff Code
2934.99.03.00
Biological target:
CX08005 is a competitive PTP1B inhibitor (IC50 = 0.781 μM).
In vitro activity:
CX08005 exhibited remarkable dose‐dependent inhibitory activity against PTP1B with an IC50 of 7.81 × 10−7 M (Figure 1B).
Reference: Br J Pharmacol. 2016 Jun; 173(12): 1939–1949. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4882499/.
In vivo activity:
CX08005 was tested in KKAy mice, which is a genetic model of T2DM. KKAy mice exhibited a higher level of glucose and insulin in response to the GTT. The two parameters were much higher in KKAy mice than in control mice in GTT (Figure 4A–D). After CX08005 treatment, GTT was improved significantly with 37.0% decrease in AUCglucose (Figure 4B).
Reference: Br J Pharmacol. 2016 Jun; 173(12): 1939–1949. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC4882499/.
|
Solvent |
mg/mL |
mM |
Solubility |
DMSO |
45.4 |
100.00 |
Ethanol |
45.4 |
100.00 |
Note: There can be variations in solubility for the same chemical from different vendors or different batches from the same vendor. The following factors can affect the solubility of the same chemical: solvent used for crystallization, residual solvent content, polymorphism, salt versus free form, degree of hydration, solvent temperature. Please use the solubility data as a reference only. Warming and sonication will facilitate dissolving. Still have questions? Please contact our Technical Support scientists.
Preparing Stock Solutions
The following data is based on the
product
molecular weight
453.62
Batch specific molecular weights may vary
from batch to batch
due to the degree of hydration, which will
affect the solvent
volumes required to prepare stock solutions.
Concentration / Solvent Volume / Mass |
1 mg |
5 mg |
10 mg |
1 mM |
1.15 mL |
5.76 mL |
11.51 mL |
5 mM |
0.23 mL |
1.15 mL |
2.3 mL |
10 mM |
0.12 mL |
0.58 mL |
1.15 mL |
50 mM |
0.02 mL |
0.12 mL |
0.23 mL |
Formulation protocol:
1. Zhang X, Tian J, Li J, Huang L, Wu S, Liang W, Zhong L, Ye J, Ye F. A novel protein tyrosine phosphatase 1B inhibitor with therapeutic potential for insulin resistance. Br J Pharmacol. 2016 Jun;173(12):1939-49. doi: 10.1111/bph.13483. Epub 2016 May 4. PMID: 26990621; PMCID: PMC4882499.
In vitro protocol:
1. Zhang X, Tian J, Li J, Huang L, Wu S, Liang W, Zhong L, Ye J, Ye F. A novel protein tyrosine phosphatase 1B inhibitor with therapeutic potential for insulin resistance. Br J Pharmacol. 2016 Jun;173(12):1939-49. doi: 10.1111/bph.13483. Epub 2016 May 4. PMID: 26990621; PMCID: PMC4882499.
In vivo protocol:
1. Zhang X, Tian J, Li J, Huang L, Wu S, Liang W, Zhong L, Ye J, Ye F. A novel protein tyrosine phosphatase 1B inhibitor with therapeutic potential for insulin resistance. Br J Pharmacol. 2016 Jun;173(12):1939-49. doi: 10.1111/bph.13483. Epub 2016 May 4. PMID: 26990621; PMCID: PMC4882499.
1: Zhang X, Tian J, Li J, Huang L, Wu S, Liang W, Zhong L, Ye J, Ye F. A novel protein tyrosine phosphatase 1B inhibitor with therapeutic potential for insulin resistance. Br J Pharmacol. 2016 Jun;173(12):1939-49. doi: 10.1111/bph.13483. Epub 2016 May 4. PubMed PMID: 26990621; PubMed Central PMCID: PMC4882499.
Qiu J, Bosch MA, Zhang C, Rønnekleiv OK, Kelly MJ. Estradiol Protects Neuropeptide Y/Agouti-Related Peptide Neurons against Insulin Resistance in Females. Neuroendocrinology. 2020;110(1-2):105-118. doi: 10.1159/000501560. Epub 2019 Jun 19. PMID: 31212279; PMCID: PMC6920578.
Li J, Zhang X, Tian J, Li J, Li X, Wu S, Liu Y, Han J, Ye F. CX08005, a Protein Tyrosine Phosphatase 1B Inhibitor, Attenuated Hepatic Lipid Accumulation and Microcirculation Dysfunction Associated with Nonalcoholic Fatty Liver Disease. Pharmaceuticals (Basel). 2023 Jan 11;16(1):106. doi: 10.3390/ph16010106. PMID: 36678603; PMCID: PMC9863901.