WARNING: This product is for research use only, not for human or veterinary use.
MedKoo CAT#: 526695
CAS#: 186544-26-3 (free base)
Description: LY-344864 is a potent 5-HT1 receptor agonist.
MedKoo Cat#: 526695
Name: LY-344864 free base
CAS#: 186544-26-3 (free base)
Chemical Formula: C21H22FN3O
Exact Mass: 351.1747
Molecular Weight: 351.4254
Elemental Analysis: C, 71.77; H, 6.31; F, 5.41; N, 11.96; O, 4.55
Related CAS #: 1217756-94-9 (HCl) 186544-26-3 (free base)
Synonym: LY-344864; LY344864; LY 344864 free base
IUPAC/Chemical Name: N-[(3R)-3-(Dimethylamino)-2,3,4,9-tetrahydro-1H-carbazol-6-yl]-4-fluorobenzamide
InChi Key: GKWHICIUSVVNGX-MRXNPFEDSA-N
InChi Code: InChI=1S/C21H22FN3O/c1-25(2)16-8-10-20-18(12-16)17-11-15(7-9-19(17)24-20)23-21(26)13-3-5-14(22)6-4-13/h3-7,9,11,16,24H,8,10,12H2,1-2H3,(H,23,26)/t16-/m1/s1
SMILES Code: O=C(NC1=CC2=C(NC3=C2C[C@H](N(C)C)CC3)C=C1)C4=CC=C(F)C=C4
Appearance: Solid powder
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, not in water
Shelf Life: >2 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: 2934.99.9001
| Biological target: | LY 344864 is a selective, orally active 5-HT1F receptor agonist with a Ki of 6 nM. |
| In vitro activity: | LY344864 is a selective receptor agonist with an affinity of 6 nM (Ki) at the recently cloned 5-HT1F receptor. When examined for its ability to inhibit forskolin-induced cyclic AMP accumulation in cells stably transfected with human 5-HT1F receptors, LY344864 was shown to be a full agonist producing an effect similar in magnitude to serotonin itself. Reference: Life Sci. 1997;61(21):2117-26. https://pubmed.ncbi.nlm.nih.gov/9395253/ |
| In vivo activity: | Increased mitochondrial DNA content and nuclear- and mitochondrial-encoded mRNA and protein expression was observed in specific brain regions of LY344864-treated naïve and lesioned mice, indicating augmented MB. LY344864 attenuated TH-ir loss in the striatum and substantia nigra compared to vehicle-treated lesioned animals. LY344864 treatment also increased locomotor activity in 6-hydroxydopamine lesioned mice, while vehicle treatment had no effect. Reference: Br J Pharmacol. 2018 Jan;175(2):348-358. https://pubmed.ncbi.nlm.nih.gov/29057453/ |
| Solvent | Max Conc. mg/mL | Max Conc. mM | |
|---|---|---|---|
| Solubility | |||
| DMSO | 100.0 | 284.56 |
The following data is based on the product molecular weight 351.4254 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. Bhargava P, Janda J, Schnellmann RG. Elucidation of cGMP-dependent induction of mitochondrial biogenesis through PKG and p38 MAPK in the kidney. Am J Physiol Renal Physiol. 2020 Feb 1;318(2):F322-F328. doi: 10.1152/ajprenal.00533.2019. Epub 2019 Dec 16. PMID: 31841384; PMCID: PMC7052650. 2. Phebus LA, Johnson KW, Zgombick JM, Gilbert PJ, Van Belle K, Mancuso V, Nelson DL, Calligaro DO, Kiefer AD Jr, Branchek TA, Flaugh ME. Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brain penetration and activity in the neurogenic dural inflammation model of migraine. Life Sci. 1997;61(21):2117-26. doi: 10.1016/s0024-3205(97)00885-0. PMID: 9395253. 3. Saengjaroentham C, Strother LC, Dripps I, Sultan Jabir MR, Pradhan A, Goadsby PJ, Holland PR. Differential medication overuse risk of novel anti-migraine therapeutics. Brain. 2020 Sep 1;143(9):2681-2688. doi: 10.1093/brain/awaa211. PMID: 32810212; PMCID: PMC7523700. 4. Scholpa NE, Lynn MK, Corum D, Boger HA, Schnellmann RG. 5-HT1F receptor-mediated mitochondrial biogenesis for the treatment of Parkinson's disease. Br J Pharmacol. 2018 Jan;175(2):348-358. doi: 10.1111/bph.14076. Epub 2017 Dec 22. PMID: 29057453; PMCID: PMC5758398. |
| In vitro protocol: | 1. Bhargava P, Janda J, Schnellmann RG. Elucidation of cGMP-dependent induction of mitochondrial biogenesis through PKG and p38 MAPK in the kidney. Am J Physiol Renal Physiol. 2020 Feb 1;318(2):F322-F328. doi: 10.1152/ajprenal.00533.2019. Epub 2019 Dec 16. PMID: 31841384; PMCID: PMC7052650. 2. Phebus LA, Johnson KW, Zgombick JM, Gilbert PJ, Van Belle K, Mancuso V, Nelson DL, Calligaro DO, Kiefer AD Jr, Branchek TA, Flaugh ME. Characterization of LY344864 as a pharmacological tool to study 5-HT1F receptors: binding affinities, brain penetration and activity in the neurogenic dural inflammation model of migraine. Life Sci. 1997;61(21):2117-26. doi: 10.1016/s0024-3205(97)00885-0. PMID: 9395253. |
| In vivo protocol: | 1. Saengjaroentham C, Strother LC, Dripps I, Sultan Jabir MR, Pradhan A, Goadsby PJ, Holland PR. Differential medication overuse risk of novel anti-migraine therapeutics. Brain. 2020 Sep 1;143(9):2681-2688. doi: 10.1093/brain/awaa211. PMID: 32810212; PMCID: PMC7523700. 2. Scholpa NE, Lynn MK, Corum D, Boger HA, Schnellmann RG. 5-HT1F receptor-mediated mitochondrial biogenesis for the treatment of Parkinson's disease. Br J Pharmacol. 2018 Jan;175(2):348-358. doi: 10.1111/bph.14076. Epub 2017 Dec 22. PMID: 29057453; PMCID: PMC5758398. |
