Lu AF21934
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Hodoodo CAT#: H530464

CAS#: 1445605-23-1

Description: Lu AF21934 is a positive allosteric modulator of mGlu4 receptors. Lu AF21934 reduces the harmaline-induced hyperactivity but not tremor in rats. The actions of Lu AF21934 are 5-HT1A receptor-dependent. Activation of the mGlu4 receptor may be a promising mechanism for the development of novel antipsychotic drugs, efficacious toward positive, negative, and cognitive symptoms.


Chemical Structure

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Lu AF21934
CAS# 1445605-23-1

Theoretical Analysis

Hodoodo Cat#: H530464
Name: Lu AF21934
CAS#: 1445605-23-1
Chemical Formula: C14H16Cl2N2O2
Exact Mass: 314.06
Molecular Weight: 315.194
Elemental Analysis: C, 53.35; H, 5.12; Cl, 22.49; N, 8.89; O, 10.15

Price and Availability

Size Price Availability Quantity
10mg USD 150 Ready to ship
25mg USD 250 Ready to ship
50mg USD 450 Ready to ship
100mg USD 750 Ready to ship
200mg USD 1250 Ready to ship
500mg USD 1950 Ready to ship
1g USD 3250 Ready to ship
2g USD 5850 2 Weeks
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Synonym: Lu AF21934; Lu AF-21934; Lu AF 21934; Lu-AF21934; Lu-AF-21934; Lu-AF 21934; LuAF21934; LuAF-21934; LuAF 21934;

IUPAC/Chemical Name: (1S,2R)-N1-(3,4-Dichlorophenyl)cyclohexane-1,2-dicarboxamide

InChi Key: AVKZWCJNDWOBAM-ZJUUUORDSA-N

InChi Code: InChI=1S/C14H16Cl2N2O2/c15-11-6-5-8(7-12(11)16)18-14(20)10-4-2-1-3-9(10)13(17)19/h5-7,9-10H,1-4H2,(H2,17,19)(H,18,20)/t9-,10+/m1/s1

SMILES Code: O=C([C@@H]1[C@H](C(N)=O)CCCC1)NC2=CC=C(Cl)C(Cl)=C2

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

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

More Info:

Biological target: Lu AF21934 is a selective and brain-penetrant mGlu4 receptor positive allosteric modulator with an EC50 of 500 nM.
In vitro activity: TBD
In vivo activity: This study reports follow-up investigations on the mechanism of action of Lu AF21934, focusing on the functional interaction between the mGlu4 and 5-hydroxytryptamine (HT)1A receptors in rodents. Lu AF21934 administered at a dose of 1 mg/kg, s.c, induced a clear antipsychotic-like effect, reversing MK-801-induced hyperactivity (P < 0.009). Lu AF21934 administered at a dose of 2 mg/kg significantly inhibited the number of DOI-induced head twitches (P < 0.01). Lu AF21934 was given at a dose of 0.5 mg/kg, 60 min before the social interaction test in rats. The compound reversed social deficits induced by MK-801 administration (number of social contacts and the total duration of contacts, P < 0.0002). Lu AF21934 was administered at a dose of 5 mg/kg, 60 min before the novel object recognition test in rats, increasing the recognition index disturbed by MK-801 administration (P < 0.005). Lu AF21934 was given at a dose of 5 mg/kg, 60 min before the spatial delayed alternation test in rats, inducing antipsychotic-like effects in the spatial delayed alteration (SDA) paradigm (P < 0.0007). Newman-Keuls comparison revealed that WAY100635 antagonized Lu AF21934-induced effect, P < 0.0007, comparing to Lu AF21934-treated animals (Fig. 7a). In our present studies, the actions of Lu AF21934 were inhibited by WAY100635 in all tests conducted, suggesting that in these models, 5-HT1A receptors play an important mechanistic role in the expression of Lu AF21934-mediated effects, independently of the mechanism of mGlu4 receptor activation. Reference: Br J Pharmacol. 2013 Aug;169(8):1824-39. https://pubmed.ncbi.nlm.nih.gov/23714045/

Solubility Data

Solvent Max Conc. mg/mL Max Conc. mM
Solubility
DMSO 55.0 174.50

Preparing Stock Solutions

The following data is based on the product molecular weight 315.19 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.

Recalculate based on batch purity %
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. Ossowska K, Wardas J, Berghauzen-Maciejewska K, Głowacka U, Kuter K, Pilc A, Zorn SH, Doller D. Lu AF21934, a positive allosteric modulator of mGlu4 receptors, reduces the harmaline-induced hyperactivity but not tremor in rats. Neuropharmacology. 2014 Aug;83:28-35. doi: 10.1016/j.neuropharm.2014.03.018. Epub 2014 Apr 12. PMID: 24726309. 2. Wierońska JM, Sławińska A, Łasoń-Tyburkiewicz M, Gruca P, Papp M, Zorn SH, Doller D, Kłeczek N, Noworyta-Sokołowska K, Gołembiowska K, Pilc A. The antipsychotic-like effects in rodents of the positive allosteric modulator Lu AF21934 involve 5-HT1A receptor signaling: mechanistic studies. Psychopharmacology (Berl). 2015 Jan;232(1):259-73. doi: 10.1007/s00213-014-3657-4. Epub 2014 Jul 11. PMID: 25012236; PMCID: PMC4281359.
In vitro protocol: TBD
In vivo protocol: 1. Ossowska K, Wardas J, Berghauzen-Maciejewska K, Głowacka U, Kuter K, Pilc A, Zorn SH, Doller D. Lu AF21934, a positive allosteric modulator of mGlu4 receptors, reduces the harmaline-induced hyperactivity but not tremor in rats. Neuropharmacology. 2014 Aug;83:28-35. doi: 10.1016/j.neuropharm.2014.03.018. Epub 2014 Apr 12. PMID: 24726309. 2. Wierońska JM, Sławińska A, Łasoń-Tyburkiewicz M, Gruca P, Papp M, Zorn SH, Doller D, Kłeczek N, Noworyta-Sokołowska K, Gołembiowska K, Pilc A. The antipsychotic-like effects in rodents of the positive allosteric modulator Lu AF21934 involve 5-HT1A receptor signaling: mechanistic studies. Psychopharmacology (Berl). 2015 Jan;232(1):259-73. doi: 10.1007/s00213-014-3657-4. Epub 2014 Jul 11. PMID: 25012236; PMCID: PMC4281359.

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1: Wierońska JM, Sławińska A, Łasoń-Tyburkiewicz M, Gruca P, Papp M, Zorn SH, Doller D, Kłeczek N, Noworyta-Sokołowska K, Gołembiowska K, Pilc A. The antipsychotic-like effects in rodents of the positive allosteric modulator Lu AF21934 involve 5-HT1A receptor signaling: mechanistic studies. Psychopharmacology (Berl). 2015 Jan;232(1):259-73. doi: 10.1007/s00213-014-3657-4. PubMed PMID: 25012236; PubMed Central PMCID: PMC4281359.

2: Sławińska A, Wierońska JM, Stachowicz K, Pałucha-Poniewiera A, Uberti MA, Bacolod MA, Doller D, Pilc A. Anxiolytic- but not antidepressant-like activity of Lu AF21934, a novel, selective positive allosteric modulator of the mGlu₄ receptor. Neuropharmacology. 2013 Mar;66:225-35. doi: 10.1016/j.neuropharm.2012.05.001. PubMed PMID: 22634361.

3: Ossowska K, Wardas J, Berghauzen-Maciejewska K, Głowacka U, Kuter K, Pilc A, Zorn SH, Doller D. Lu AF21934, a positive allosteric modulator of mGlu4 receptors, reduces the harmaline-induced hyperactivity but not tremor in rats. Neuropharmacology. 2014 Aug;83:28-35. doi: 10.1016/j.neuropharm.2014.03.018. PubMed PMID: 24726309.

4: Sławińska A, Wierońska JM, Stachowicz K, Marciniak M, Lasoń-Tyburkiewicz M, Gruca P, Papp M, Kusek M, Tokarski K, Doller D, Pilc A. The antipsychotic-like effects of positive allosteric modulators of metabotropic glutamate mGlu4 receptors in rodents. Br J Pharmacol. 2013 Aug;169(8):1824-39. doi: 10.1111/bph.12254. PubMed PMID: 23714045; PubMed Central PMCID: PMC3753838.

5: Bennouar KE, Uberti MA, Melon C, Bacolod MD, Jimenez HN, Cajina M, Kerkerian-Le Goff L, Doller D, Gubellini P. Synergy between L-DOPA and a novel positive allosteric modulator of metabotropic glutamate receptor 4: implications for Parkinson's disease treatment and dyskinesia. Neuropharmacology. 2013 Mar;66:158-69. doi: 10.1016/j.neuropharm.2012.03.022. PubMed PMID: 22491024.

6: Gubellini P, Melon C, Dale E, Doller D, Kerkerian-Le Goff L. Distinct effects of mGlu4 receptor positive allosteric modulators at corticostriatal vs. striatopallidal synapses may differentially contribute to their antiparkinsonian action. Neuropharmacology. 2014 Oct;85:166-77. doi: 10.1016/j.neuropharm.2014.05.025. PubMed PMID: 24866785.

7: Zaniewska M, Przegaliński E, Filip M, Pilc A, Doller D. Inhibitory actions of mGlu4 receptor ligands on cocaine-, but not nicotine-, induced sensitizing and conditioning locomotor responses in rats. Pharmacol Rep. 2014 Apr;66(2):205-11. doi: 10.1016/j.pharep.2013.12.001. PubMed PMID: 24911071.

8: Nickols HH, Conn PJ. Development of allosteric modulators of GPCRs for treatment of CNS disorders. Neurobiol Dis. 2014 Jan;61:55-71. doi: 10.1016/j.nbd.2013.09.013. Review. PubMed PMID: 24076101; PubMed Central PMCID: PMC3875303.