JTC-801

Catalog No.S2722 Batch:S272201

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Technical Data

Formula

C26H25N3O2.HCl
Molecular Weight 447.96 CAS No. 244218-51-7
Solubility (25°C)* In vitro DMSO 90 mg/mL (200.91 mM)
Ethanol 31 mg/mL (69.2 mM)
Water Insoluble
In vivo (Add solvents to the product individually and in order)
Homogeneous suspension
CMC-NA
≥5mg/ml Taking the 1 mL working solution as an example, add 5 mg of this product to 1 ml of CMC-Na solution, mix evenly to obtain a homogeneous suspension with a final concentration of 5 mg/ml.
Homogeneous suspension
0.5% methylcellulose

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 10.000mg/ml (22.32mM) Taking the 1 mL working solution as an example, take 10 mg of this product, add it to 1 ml of 0.5% methylcellulose clear solution, and mix evenly to form a uniform suspension. The mixed solution should be used immediately for optimal results. 
Clear solution
5%DMSO 40%PEG300 5%Tween80 50%ddH2O

Validated by Selleck labs. Should you need adjustments to this formulation, contact our sales team for custom testing.

 5.000mg/ml (11.16mM) Taking the 1 mL working solution as an example, add 50 μL of 100 mg/ml clarified DMSO stock solution to 400 μL of PEG300, mix evenly to clarify it; add 50 μL of Tween80 to the above system, mix evenly to clarify; then continue to add 500 μL of ddH2O to adjust the volume to 1 mL. The mixed solution should be used immediately for optimal results. 
* <1 mg/ml means slightly soluble or insoluble.
* Please note that Selleck tests the solubility of all compounds in-house, and the actual solubility may differ slightly from published values. This is normal and is due to slight batch-to-batch variations.
* Room temperature shipping (Stability testing shows this product can be shipped without any cooling measures.)

Preparing Stock Solutions

Biological Activity

Description JTC-801 is a selective opioid receptor-like1 (ORL1) receptor antagonist with IC50 of 94 nM, weakly inhibits receptors δ, κ, and μ.
Targets
Opioid receptor-like1 (ORL1) [1]
94 nM
In vitro JTC-801 displays about 12.5-, 129-, and 1055-fold selectivity for ORL1 receptor (Ki = 8.2 nM) over μ-, κ-, and δ-opioid receptors, respectively. This compound does not inhibit forskolin-stimulated cyclic AMP accumulation in human ORL1 receptor-expressing HeLa cells, but it prevents nociceptin-induced inhibition of cyclic AMP accumulation, indicating that this chemical possesses full antagonistic activity. [2] In rat cerebrocortical membrane, this compound inhibits ORL1 receptor with IC50 of 472 nM and μ-receptor with IC50 of 1831 nM. It completely antagonizes the suppression of nociceptin on forskolin-induced accumulation of cyclic AMP with IC50 of 2.58 μM in HeLa cells expressing ORL1 receptor. [1]
In vivo Oral administration of JTC-801 (0.3-3 mg/kg) antagonizes nociceptin-induced allodynia in mice, and shows analgesic effect in a hot plate test using mice and in a formalin test using rats. [2] In mouse hot-plate test, this compound prolongs escape response latency (ERL) or exposed heat stimulus with minimum effective doses (MED) of 0.01 mg/kg by i.v. or 1 mg/kg by p.o. In the rat formalin test, it reduces both the first and second phases of the nociceptive response with MED of 0.01 mg/kg71 by i.v. or 1 mg/kg by p.o. [1] This chemical dose-dependently normalizes paw withdrawal latency (PWL). Although it does not inhibit a chronic constriction injury (CCI)-induced decrease in bone mineral content (BMC) and bone mineral density (BMD), it inhibits an increase in the number of osteoclasts. [3] Tactile allodynia induced by L5/L6 spinal nerve ligation is reversed by both systemic (3-30 mg/kg) and spinal (22.5 and 45 pg) administration of this compound in a dose-dependent manner. Furthermore, systemic treatment reduces Fos-like immunoreactivity in the dorsal horn of the spinal cord (laminae I/II). [4] It produces dose-dependent mechanical and cold anti-allodynic effects with ED50 of 0.83 mg/kg and 1.02 mg/kg, respectively. [6]

Protocol (from reference)

Animal Study:

[1]
  • Animal Models

    Male ICR (CD-1) subjected to nociceptin-induced allodynia test or hot plate test, and Male SD rats subjected to formalin-induced paw-licking response

  • Dosages

    ~10 mg/kg

  • Administration

    Orally or injected i.v.

References

  • https://pubmed.ncbi.nlm.nih.gov/11815367/
  • https://pubmed.ncbi.nlm.nih.gov/11101358/
  • https://pubmed.ncbi.nlm.nih.gov/14623124/
  • https://pubmed.ncbi.nlm.nih.gov/15763246/
  • https://pubmed.ncbi.nlm.nih.gov/17512052/
  • https://pubmed.ncbi.nlm.nih.gov/21664922/

Customer Product Validation

<p>The effects of JTC-801, chloroquine phosphate, and SCF antibody on the expression of collagen type I in the dorsal skin of tranexamic acid-treated NOA mice. The values are expressed as the mean ± SD derived from 10 animals. *p < 0.05.</p>

, , Antimicrob Agents Chemother, 2016, 60(6):3813-6.

The effect of JTC-801 and naltrexone. (B) plasma IL-6 and (C) plasma TNF-α concentrations in the colon carcinoma model. The values represent the mean±SD derived from 6 animals. *, P<0.05

Data from [ , , Photodermatol Photoimmunol Photomed, 2017, 33(2):84-91 ]

The effects of JTC-801 and RU486 on the colitis score, body weight and length of the large intestine of the UVB/DSS-treated (A, B, C) andUVA/DSS-treated mice (D, E, F). The values represent the means±SD (C, F) and pooled SEM (A, B, D, E). *P < 0.05.

Data from [ , , Photochem Photobiol, 2016, 92(5):728-34. ]

Selleck's JTC-801 Has Been Cited by 11 Publications

Cryptotanshinone differentially induces cell death in ATP6V0D1-deficient pancreatic cancer cells [ Cancer Drug Resist, 2025, 8:45] PubMed: 41019981
Ciprofloxacin is a novel anti-ferroptotic antibiotic [ Heliyon, 2024, 10(11):e32571] PubMed: 38961954
ACSS2-mediated NF-κB activation promotes alkaliptosis in human pancreatic cancer cells [ Sci Rep, 2023, 13(1):1483] PubMed: 36707625
ACSS2-mediated NF-κB activation promotes alkaliptosis in human pancreatic cancer cells [ Sci Rep, 2023, 13(1):1483] PubMed: 36707625
A compendium of kinetic modulatory profiles identifies ferroptosis regulators [ Nat Chem Biol, 2021, 10.1038/s41589-021-00751-4] PubMed: 33686292
Targeting NF-κB-dependent alkaliptosis for the treatment of venetoclax-resistant acute myeloid leukemia cells [ Biochem Biophys Res Commun, 2021, 562:55-61] PubMed: 34034094
Ultraviolet A eye irradiation ameliorates colon carcinoma induced by azoxymethane and dextran sodium sulfate through β‐endorphin and methionine‐enkephalin [Hiramoto K, et al. Photodermatol Photoimmunol Photomed, 2017, 33(2):84-91] PubMed: 28039905
The amelioration effect of tranexamic acid in wrinkles induced by skin dryness [Hiramoto K, et al. Biomedicine & Pharmacotherapy, 2016, 80:16-22]
The amelioration effect of tranexamic acid in wrinkles induced by skin dryness [ Biomed Pharmacother, 2016, 80:16-22] PubMed: 27133035
The amelioration effect of tranexamic acid in wrinkles induced by skin dryness. [ Biomed Pharmacother, 2016, 80:16-22] PubMed: 27133035

RETURN POLICY
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SHIPPING AND STORAGE
Selleck products are transported at room temperature. If you receive the product at room temperature, please rest assured, the Selleck Quality Inspection Department has conducted experiments to verify that the normal temperature placement of one month will not affect the biological activity of powder products. After collecting, please store the product according to the requirements described in the datasheet. Most Selleck products are stable under the recommended conditions.

NOT FOR HUMAN, VETERINARY DIAGNOSTIC OR THERAPEUTIC USE.