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MW 411.9 Da, Purity >98%. Highly potent, selective, competitive, non-peptide CCK1 receptor antagonist (Ki = 0.2 nM). Increases plasma leptin levels. Shows central effects. Stimulates food intake *in vivo.* Orally active.

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Key facts

CAS number
136381-85-6
Purity
> 98%
Form
Solid
Molecular weight
411.9 Da
Molecular formula
C20H14ClN3O3S
PubChem identifier
122077
Nature
Synthetic

Alternative names

Recommended products

MW 411.9 Da, Purity >98%. Highly potent, selective, competitive, non-peptide CCK1 receptor antagonist (Ki = 0.2 nM). Increases plasma leptin levels. Shows central effects. Stimulates food intake *in vivo.* Orally active.

Key facts

Purity
> 98%
PubChem identifier
122077
Solubility

Soluble in DMSO to 100 mM.

Biochemical name
Lintitript
Biological description

Highly potent, selective, competitive, non-peptide CCK1 receptor antagonist (Ki = 0.2 nM). Increases plasma leptin levels. Shows central effects. Stimulates food intake *in vivo.* Orally active.

Canonical SMILES
C1=CC=C2C(=C1)C=C(N2CC(=O)O)C(=O)NC3=NC(=CS3)C4=CC=CC=C4Cl
InChI
InChI=1S/C20H14ClN3O3S/c21-14-7-3-2-6-13(14)15-11-28-20(22-15)23-19(27)17-9-12-5-1-4-8-16(12)24(17)10-18(25)26/h1-9,11H,10H2,(H,25,26)(H,22,23,27)
InChIKey
ILNRQFBVVQUOLP-UHFFFAOYSA-N
IUPAC name
2-[2-[[4-(2-chlorophenyl)-1,3-thiazol-2-yl]carbamoyl]indol-1-yl]acetic acid

Storage

Shipped at conditions
Ambient - Can Ship with Ice
Appropriate short-term storage conditions
+4°C
Appropriate long-term storage conditions
+4°C
Storage information
The product can be stored for up to 12 months

Supplementary info

This supplementary information is collated from multiple sources and compiled automatically.
Activity summary

The c-Jun protein also known as AP-1 is a transcription factor with a molecular weight of approximately 39 kDa. It is widely expressed in various tissues particularly in neurons where it plays a role in gene regulation. Vitamin D Receptor (VDR) a nuclear receptor of about 48 kDa binds with vitamin D to regulate calcium homeostasis and is mainly found in the intestines bones and kidneys. PPAR gamma 2 involved in adipocyte differentiation weighs around 57 kDa and expresses mainly in adipose tissue. The Pregnane X Receptor (PXR) approximately 50 kDa is a nuclear receptor found in the liver and small intestine important for xenobiotic metabolism. TRH-R or thyrotropin-releasing hormone receptor and CCK1-R or cholecystokinin receptor are membrane-bound receptors involved in hormone signaling primarily in the central nervous system and gastrointestinal tract. USP1 is an ubiquitin-specific protease critical for protein degradation pathways frequently found in proliferating cells. Lastly Nrf2 acts as a regulator of antioxidant proteins and expresses in many cell types under stress conditions.

Biological function summary

These proteins influence substantial aspects of cellular function and metabolism. c-Jun forms part of the AP-1 complex impacting cellular proliferation and apoptosis. Vitamin D Receptor modulates gene expression related to immune responses and bone development. PPAR gamma 2 influences fat storage and glucose metabolism. PXR regulates the expression of enzymes involved in drug metabolism. TRH-R and CCK1-R transmit signals essential for hormone-mediated physiological responses. USP1 contributes to DNA repair and maintaining genomic stability. Nrf2 when activated translocates to the nucleus to initiate the transcription of antioxidant response genes working alongside enzymes such as HO-1.

Pathways

These proteins integrate into significant metabolic and regulatory networks. c-Jun influences the MAPK signaling pathway associating closely with proteins like JNK. Vitamin D Receptor plays an important role in the calcium signaling pathway and interacts with retinoid X receptors. PPAR gamma 2 aligns with adipogenesis pathways and cross-talks with insulin signaling. PXR integrates into the detoxification pathway often synergizing with cytochrome P450 enzymes. TRH-R and CCK1-R operate within the neuroendocrine signaling pathways. USP1 functions within the DNA damage response pathway working with PCNA and FANCD2. Nrf2 is principally involved in the oxidative stress pathway collaborating with proteins like KEAP1.

Associated diseases and disorders

These proteins have strong links to various health conditions. Dysfunctional c-Jun activity associates with neurodegenerative diseases including Alzheimer's as it affects neuron survival. Vitamin D Receptor impairment connects to bone disorders like rickets. PPAR gamma 2 mutations can result in metabolic syndromes such as diabetes linked with insulin resistance proteins. PXR variations might influence susceptibility to liver diseases through altered metabolism. Abnormal TRH-R and CCK1-R signaling can contribute to psychiatric disorders and digestive problems respectively. USP1 mutations are associated with cancer given its role in genomic stability. Aberrant Nrf2 function connects to chronic inflammatory conditions by altering stress response pathways.

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