CIVENTICHEM CV-4057 Property

Melting point:

201 °C (decomp)

Boiling point:

484.8±45.0 °C(Predicted)

Density 

1.395±0.06 g/cm3(Predicted)

storage temp. 

Sealed in dry,Room Temperature

solubility 

Soluble in DMSO (>25 mg/ml)

form 

solid

pka

4.50±1.00(Predicted)

color 

Off-white

Stability:

Stable for 2 years from date of purchase as supplied. Solutions in DMSO may be stored at -20°C for up to 3 months.

Safety

Hazard Codes 

T

Risk Statements 

25

Safety Statements 

45

RIDADR 

UN 2811 6.1 / PGIII

Hazard and Precautionary Statements (GHS)

Symbol(GHS)

Signal word

Danger

Hazard statements

H301Toxic if swalloed

Precautionary statements

P301+P310IF SWALLOWED: Immediately call a POISON CENTER or doctor/physician.

CIVENTICHEM CV-4057 Chemical Properties,Usage,Production

Description

Laquinimod (248281-84-7) is an immunomodulator1 that inhibits inflammation2 and autoimmunity3,4 via activation of the aryl hydrocarbon receptor (AhR)5. It has been investigated as a treatment for multiple sclerosis6 and has shown efficacy in Huntington’s disease models7,8.

Definition

ChEBI: Laquinimod is an aromatic amide.

in vitro

abr-215062 was shown to completely inhibit the development of murine acute experimental autoimmune encephalomyelitis (eae) [1].

in vivo

abr-215062 dose-dependently inhibited disease and showed better disease inhibitory effects as compared to roquinimex (linomide). furthermore, abr-215062 inhibited the inflammation of both cd4+ t cells and macrophages into central nervous tissues [2].

References

J?nsson et al. (2004), Synthesis and Biological Evaluation of New 1,2-Dihydro-4-hydroxy-2-oxo-3-quinolinecarboxamides for Treatment of Autoimmune Disorders: Structure-Activity Relationship; Med. Chem. 47 2075 Rothhammer et al. (2021); Aryl Hydrocarbon Receptor Activation in Astrocytes by Laquinimod Ameliorates Autoimmune Inflammation in the CNS, Neurol. Neuroimmunol. Neuroinflamm., 8 e946 Pitarokoili et al. (2014), Laquinimod exerts strong clinical and immunomodulatory effects in Lewis rat experimental autoimmune neuritis; Neuroimmunol., 274 38 Ott et al. (2019), Laquinimod, a prototypic quinoline-3-carboxamide and aryl hydrocarbon receptor agonist, utilizes CD155-mediated natural killer/dendritic cell interaction to suppress CNS autoimmunity; Neuroinflammation, 16 49 Kaye et al. (2016), Laquinimod arrests experimental autoimmune encephalitis by activating the aryl hydrocarbon receptor; Natl. Acad. Sci. USA., 113 E6145 Th?ne and Linker (2016), Laquinimod in the treatment of multiple sclerosis: a review of the data so far; Drug Des. Devel. Ther., 10 1111 Dobson et al. (2016), Laquinimod dampens hyperactive cytokine production in Huntington’s disease patient myeloid cells; Neurochem., 137 782 Garcia-Miralles et al. (2016), Laquinimod rescues striatal, cortical and white matter pathology and results in modest behavioural improvements in the YAC128 model of Huntington disease; Rep., 6 31652