Cellagen Technology LLC
 
작성일 : 16-10-11
[Cellagen Technology LLC] Disease Area, Immunology I
ABR-215062 (Laquinimod) | Immunomodulator / Alcaftadine | Histamine (H1/H4) receptor antagonist / AS-605240 | PI3K inhibitor / CGS-21680 | A2A receptor agonist

 

Disease Area, Immunology I

 

 

Product Name: ABR-215062 (Laquinimod) l Immunomodulator

 

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Laquinimod is an orally-available. quinolinone-based, broad spectrum immunomodulator with anti-

inflammatory activity, most likely by effecting a T-helper cell 1 to 2 cytokine shift. [1] Additionally it reduces

antigen presentation and the effect on migration of T-cells. Laquinimod is also believed to provide a

neuroprotective effect and may have application to relapsing-remitting multiple sclerosis (RRMS).

 

In animal models for multiple sclerosis, Laquinimod reversed established relapsing remitting experimental

autoimmune encephalomyelitis (RR EAE) and was associated with reduced CNS inflammation, decreased

Th1 and Th17 responses, and an increase in regulatory T cells.

 

Details

Chemical Formula:

 

C19H17ClN2O3

CAS No.:

 

248281-84-7

Molecular Weight:

 

356.8

Purity:

 

> 98%

Appearance:

 

White solid

Chemical Name:

 

 

5-chloro-N-ethyl-4-hydroxy-1-methyl-2-oxo-N-phenyl-1,2-dihydroquinoline-

carboxamide

Solubility:

 

Up to 22 mM in DMSO

Synonyms:

 

ABR-215062, ABR 215062, ABR215062, Laquinimod

Storage:

 

 

For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution

at -20oC.

 

Reference:

1. "Laquinimod for relapsing-remitting multiple sclerosis" National Horizon Scaning Centre technology

    summary, Aug. 2011.

2. West et al., Profile of oral laquinimod and its potential in the treatment of multiple sclerosis. Degenerative

    Neurological Muscular Disease 2011, 1, 25-32.

3. Schulze-Topphoff et al., Laquinimod, a quinoline-3-carboxamide, induces type II myeloid cells that

    modulate central nervous system autoimmunity. PLoS ONE 2012, 7(3), e33797.

 

 

Product Name: Alcaftadine l Histamine (H1/H4) receptor antagonist

 

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Alcaftadine, a imidazobenzazepine-based antagonist of the histamine receptors, has a pKi of 8.5 and 5.8 for

the H1 receptor and H4 receptors, respectively. Additionally, Alcaftadine shows higher affinity for the H2

receptor than ketotifen

 

In support of its potent anti-inflammatory properties, Alcaftadine also exhibits modulatory action on immune

cell recruitment and mast cell stabilizing effects. Receptor binding studies revealed less significant effects

ranging from a moderate affinity for cholinergic muscarinic receptors and lower affinity for human a2A-

adrenoreceptors, serotonin 5-H51A, 5-HT2A receptors, and melanocortin MC4 receptors. [2] Furthermore,

displacement experiments showed that at concentrations up to 10 uM, Alcaftadine did not interact with other

receptors, transporters, or ion channel binding sites, including the hERG channel.

 

Details

Chemical Formula:

 

C19H21N3O

CAS No.:

 

147084-10-4

Molecular Weight:

 

307.38

Purity:

 

> 98%

Appearance:

 

White

Chemical Name:

 

 

2-(1-Methylpiperidin-4-ylidene)-4,7-diazatricyclo[8.4.0.0(3,7)]tetradeca- 1(14)

,3,5,10,12-pentaene-6-carbaldehyde

Solubility:

 

Up to 20 mM in DMSO

Synonyms:

 

Alcaftadine, 147084-10-4, Lastacaft

Storage:

 

 

For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution

at -20oC.

 

Reference:

1. Gallois-Bernois et al., Alcaftadine, a new antihistamine with combined antagonist activity at histamine H1,

    H2, and H4 receptors. J. Receptor Ligand Channel Res. 2012, 5, 9-20.

2. Namdar et al., Alcaftadine: A topical antihistamine for use in allergic conjunctivitis. Drugs of Today, 2011,

    47(12), 883-890

3. Bohets et al., Clinical Pharmacology of Alcaftadine, a Novel Antihistamine for the Prevention of Allergic

   Conjunctivitis. J. Ocular. Pharm. Ther. 2011, 27(2), 187-195.

 

 

Product Name: AS-605240 l Pl3K inhibitor

 

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AS-605420 is an orally-available, ATP competitive inihbitor of the thiazolinedione class with IC50 potency

against PI3Kg of 8 nM. It also has peripheral activity versus other PI3K isoforms of 60 nM, 270 nM, and 300

nM for alpha, beta, and delta, respectively.

 

AS-605240 has been shown to selectively block class IB PI3K signaling in cultured macrophages. Dose-

dependent treatment resulted in lowered blood glucose levels with improvement in insulin sensitivity and

glucose tolerance without adverse effect on body weight.

 

AS-605240 has also been utilized in the exploration for experimental autoimmune encephalomyelitis (EAE).

AS605420-treated mice fully recovered from EAE and experienced significantly reduced clinical and

cumulative disease scores. Histological CNS analysis revealed that AS605240 treated mice had reduced

cellular pathology in the spinal cord and reduced signs of demyelination.

 

Details

Chemical Formula:

 

C12H7N3O2S

CAS No.:

 

648450-29-7

Molecular Weight:

 

257.27

Purity:

 

> 98%

Appearance:

 

Grey

Chemical Name:

 

(Z)-5-(quinoxalin-6-ylmethylene)thiazolidine-2,4-dione

Solubility:

 

Up to 5 mM in DMSO

Synonyms:

 

AS-605240, AS605240, AS605240

Storage:

 

 

For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution

at -20oC.

 

Reference:

1. Kobayashi et al., Blockade of class IB phosphoinositide-3 kinase ameliorates obesity-induced

   inflammation and insulin resistance. Proc. Natl. Acad. Sci. 2011, 108(14), 5753-5758.

2. Comerford et al., PI3K? drives priming and survival of autoreactive CD4(+) T cells during experimental

    autoimmune encephalomyelitis. PLoSONE, 2012, 7(9), e45095

 

 

Product Name: GCS-216680 l A2A receptor agonist

 

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CGS21680, an A2A adenosine receptor agonist, is under investigation in various inflammation models for

potential novel therapies. For example, CGS21680 possesses an anti-inflammatory effect during chronic

inflammation and lessens the tissue damage associated with collagen-induced arthritis.

 

CGS21680 reduces spinal cord injury-induced phosphorylation of JNK and MAPK. It was shown also to

reduce the influx of MPO-positive leukocytes, NFkB activation, and iNOS expression. Additionally, CGS21680

reduced phosphorylation of p65 on Ser536.

 

In acute lung inflammation models, CGS21680 was shown to reduce neutrophil infiltration and thus degree of

lung injury after a carrageenan-challenge.

 

Details

Chemical Formula:

 

C23H29N7O6

CAS No.:

 

124182-57-6

Molecular Weight:

 

499.52

Purity:

 

> 98%

Appearance:

 

White 

Chemical Name:

 

 

3-[4-[2-[ [6-amino-9-[(2R,3R,4S,5S)-5-(ethylcarbamoyl)-3,4-dihydroxy-oxolan-2-

yl]purin-2-yl]amino]ethyl]phenyl]propanoic acid

Solubility:

 

Up to 100 mM in DMSO

Synonyms:

 

CGS-21680, CGS 21680, CGS21680

Storage:

 

 

For longer shelf life, store solid powder at 4oC desiccated, or store DMSO solution

at -20oC.

 

Reference:

1. Mazzon et al., CGS 21680, an agonist of the adenosine (A2A) receptor, reduces progression of murine

    type II collagen-induced arthritis. J. Rheumatol., 2011, 38(10), 2119-2129.

2. Genovese, The selective adenosine A2A receptor agonist CGS 21680 reduces JNK MAPK activation in

    oligodendrocytes in injured spinal cord. Shock, 2009, 32(6), 578-585.

3. Impellizzeri et al., CGS 21680, an agonist of the adenosine (A2A) receptor, decreases acute lung

    inflammation. Eur. J. Pharmacol. 2011, 668, 305-316

 

Ordering informations

Catalog No.

Product Name

Size

C2215

ABR-215062 (Laquinimod) | Immunomodulator

2 mg, 10 mg & 50 mg

C9601

Alcaftadine | Histamine (H1/H4) receptor antagonist

5 mg, 25 mg & 100 mg

C2760

AS-605240 | PI3K inhibitor

5 mg, 25 mg & 100 mg

C2216

CGS-21680 | A2A receptor agonist

5 mg, 25 mg & 100 mg

 

 

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