HTL14242
HTL14242 is a mGlu5 Negative Allosteric Modulator. Metabotropic glutamate receptors (mGluRs) constitute the class C of G-protein coupled receptors (GPCRs) and play a key role in glutamatergic signaling. The inhibition of mGluR5, which is mostly expressed in the striatum, hippocampus, amygdala, and frontal cortex, is therefore considered as a potential therapeutic intervention in a number of psychiatry indications, including fragile X syndrome, anxiety, and depression.
For research use only. We do not sell to patients.
Chemical Information
| Name | HTL14242 |
|---|---|
| Iupac Chemical Name | 3-chloro-5-(6-(5-fluoropyridin-2-yl)pyrimidin-4-yl)benzonitrile |
| Synonyms | HTL14242; HTL-14242; HTL 14242; HTL0014242; TMP-301 |
| Molecular Formula | C16H8ClFN4 |
| Molecular Weight | 310.71 |
| Smile | N#CC1=CC(C2=NC=NC(C3=NC=C(F)C=C3)=C2)=CC(Cl)=C1 |
| InChiKey | FQAXDSVNYVVQSE-UHFFFAOYSA-N |
| InChi | InChI=1S/C16H8ClFN4/c17-12-4-10(7-19)3-11(5-12)15-6-16(22-9-21-15)14-2-1-13(18)8-20-14/h1-6,8-9H |
| CAS Number | 1644645-32-8 |
| Related CAS |
Ordering Information
| Packaging | Price | Availability | Purity | Shipping Time |
|---|---|---|---|---|
| Bulk | Enquiry | Enquiry | Enquiry |
| Formulation | Off-white solid |
|---|---|
| Purity | 98% Min. |
| Storage | Dry, dark and at 0 - 4℃ for short term (days to weeks) or -20℃ for long term (months to years). |
| Solubility | Soluble in DMSO |
| Handling | |
| 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. |
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| Mechanism | |
| Cell study | |
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| Clinical study |
1: Christopher JA, Aves SJ, Bennett KA, Doré AS, Errey JC, Jazayeri A, Marshall
FH, Okrasa K, Serrano-Vega MJ, Tehan BG, Wiggin GR, Congreve M. Fragment and
Structure-Based Drug Discovery for a Class C GPCR: Discovery of the mGlu5
Negative Allosteric Modulator HTL14242
(3-Chloro-5-[6-(5-fluoropyridin-2-yl)pyrimidin-4-yl]benzonitrile). J Med Chem.
2015 Aug 27;58(16):6653-64. doi: 10.1021/acs.jmedchem.5b00892. PubMed PMID:
26225459.
2: Topiol S, Sabio M. 7TM X-ray structures for class C GPCRs as new
drug-discovery tools. 1. mGluR5. Bioorg Med Chem Lett. 2016 Jan 15;26(2):484-94.
doi: 10.1016/j.bmcl.2015.11.087. PubMed PMID: 26706173.
3: Tehan BG, Christopher JA. The use of conformationally thermostabilised GPCRs
in drug discovery: application to fragment, structure and biophysical techniques.
Curr Opin Pharmacol. 2016 Oct;30:8-13. doi: 10.1016/j.coph.2016.06.010. Review.
PubMed PMID: 27400445.
Chemical Structure
