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RCGD-423

Alias: RCGD-423 RCGD 423 RCGD423 Regulator of cartilage growth and differentiation (RCGD) 423
Cat No.:V13636 Purity: ≥98%
RCGD423 is a gp130 modulator that prevents articular cartilage degradation and promotes its repair.
RCGD-423
RCGD-423 Chemical Structure CAS No.: 108237-91-8
Product category: Interleukins
This product is for research use only, not for human use. We do not sell to patients.
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Purity & Quality Control Documentation

Purity: ≥98%

Product Description
RCGD423 is a gp130 modulator that prevents articular cartilage degradation and promotes its repair.
Biological Activity I Assay Protocols (From Reference)
ln Vitro
RCGD423 is a gp130 modulator that encourages cartilage healing and inhibits cartilage mobility [1].
ln Vivo
Beyond the impairment seen in the partial response meniscectomy paradigm, RCGD423 increased chondrocyte proliferation while dramatically reducing chondrocyte hypertrophy, damage, and damage. Moreover, RCGD 423 promoted cell proliferation in the mesenchyme of the lesion, reduced the delamination of cartilage matrix in newly formed cartilage, and enhanced cartilage therapy in a full-thickness osteochondral defect model [1].
References

[1]. Drug-induced modulation of gp130 signalling prevents articular cartilage degeneration and promotes repair. Ann Rheum Dis. 2018 May;77(5):760-769.

These protocols are for reference only. InvivoChem does not independently validate these methods.
Physicochemical Properties
Molecular Formula
C15H11BRN2S
Molecular Weight
331.23
Exact Mass
329.982
CAS #
108237-91-8
Related CAS #
108237-91-8
PubChem CID
4456143
Appearance
Light yellow to yellow solid powder
Density
1.5±0.1 g/cm3
Boiling Point
465.6±47.0 °C at 760 mmHg
Flash Point
235.4±29.3 °C
Vapour Pressure
0.0±1.2 mmHg at 25°C
Index of Refraction
1.695
LogP
5.25
Hydrogen Bond Donor Count
1
Hydrogen Bond Acceptor Count
3
Rotatable Bond Count
3
Heavy Atom Count
19
Complexity
275
Defined Atom Stereocenter Count
0
InChi Key
OUFYYVAASPLOAA-UHFFFAOYSA-N
InChi Code
InChI=1S/C15H11BrN2S/c16-12-6-8-13(9-7-12)17-15-18-14(10-19-15)11-4-2-1-3-5-11/h1-10H,(H,17,18)
Chemical Name
N-(4-Bromophenyl)-4-phenyl-1,3-thiazol-2-amine
Synonyms
RCGD-423 RCGD 423 RCGD423 Regulator of cartilage growth and differentiation (RCGD) 423
HS Tariff Code
2934.99.9001
Storage

Powder      -20°C    3 years

                     4°C     2 years

In solvent   -80°C    6 months

                  -20°C    1 month

Shipping Condition
Room temperature (This product is stable at ambient temperature for a few days during ordinary shipping and time spent in Customs)
Solubility Data
Solubility (In Vitro)
DMSO : ~125 mg/mL (~377.38 mM)
Solubility (In Vivo)
Solubility in Formulation 1: 6.25 mg/mL (18.87 mM) in 10% DMSO + 90% (20% SBE-β-CD in Saline) (add these co-solvents sequentially from left to right, and one by one), suspension solution; with sonication.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 62.5 mg/mL clear DMSO stock solution to 900 μL of 20% SBE-β-CD physiological saline solution and mix evenly.
Preparation of 20% SBE-β-CD in Saline (4°C,1 week): Dissolve 2 g SBE-β-CD in 10 mL saline to obtain a clear solution.

Solubility in Formulation 2: ≥ 2.67 mg/mL (8.06 mM) (saturation unknown) in 10% DMSO + 40% PEG300 + 5% Tween80 + 45% Saline (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 26.7 mg/mL clear DMSO stock solution to 400 μL PEG300 and mix evenly; then add 50 μL Tween-80 to the above solution and mix evenly; then add 450 μL normal saline to adjust the volume to 1 mL.
Preparation of saline: Dissolve 0.9 g of sodium chloride in 100 mL ddH₂ O to obtain a clear solution.

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Solubility in Formulation 3: ≥ 2.67 mg/mL (8.06 mM) (saturation unknown) in 10% DMSO + 90% Corn Oil (add these co-solvents sequentially from left to right, and one by one), clear solution.
For example, if 1 mL of working solution is to be prepared, you can add 100 μL of 26.7 mg/mL clear DMSO stock solution to 900 μL of corn oil and mix evenly.


 (Please use freshly prepared in vivo formulations for optimal results.)
Preparing Stock Solutions 1 mg 5 mg 10 mg
1 mM 3.0191 mL 15.0953 mL 30.1905 mL
5 mM 0.6038 mL 3.0191 mL 6.0381 mL
10 mM 0.3019 mL 1.5095 mL 3.0191 mL

*Note: Please select an appropriate solvent for the preparation of stock solution based on your experiment needs. For most products, DMSO can be used for preparing stock solutions (e.g. 5 mM, 10 mM, or 20 mM concentration); some products with high aqueous solubility may be dissolved in water directly. Solubility information is available at the above Solubility Data section. Once the stock solution is prepared, aliquot it to routine usage volumes and store at -20°C or -80°C. Avoid repeated freeze and thaw cycles.

Calculator

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An example of molarity calculation using the molarity calculator is shown below:
What is the mass of compound required to make a 10 mM stock solution in 5 ml of DMSO given that the molecular weight of the compound is 350.26 g/mol?
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  • The answer of 17.513 mg appears in the Mass box. In a similar way, you may calculate the volume and concentration.

Dilution Calculator allows you to calculate how to dilute a stock solution of known concentrations. For example, you may Enter C1, C2 & V2 to calculate V1, as detailed below:

What volume of a given 10 mM stock solution is required to make 25 ml of a 25 μM solution?
Using the equation C1V1 = C2V2, where C1=10 mM, C2=25 μM, V2=25 ml and V1 is the unknown:
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  • The answer of 62.5 μL (0.1 ml) appears in the Volume (Start) box
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Molecular Weight Calculator allows you to calculate the molar mass and elemental composition of a compound, as detailed below:

Note: Chemical formula is case sensitive: C12H18N3O4  c12h18n3o4
Instructions to calculate molar mass (molecular weight) of a chemical compound:
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Definitions of molecular mass, molecular weight, molar mass and molar weight:
  • Molecular mass (or molecular weight) is the mass of one molecule of a substance and is expressed in the unified atomic mass units (u). (1 u is equal to 1/12 the mass of one atom of carbon-12)
  • Molar mass (molar weight) is the mass of one mole of a substance and is expressed in g/mol.
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In vivo Formulation Calculator (Clear solution)
Step 1: Enter information below (Recommended: An additional animal to make allowance for loss during the experiment)
Step 2: Enter in vivo formulation (This is only a calculator, not the exact formulation for a specific product. Please contact us first if there is no in vivo formulation in the solubility section.)
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Calculation results

Working concentration mg/mL;

Method for preparing DMSO stock solution mg drug pre-dissolved in μL DMSO (stock solution concentration mg/mL). Please contact us first if the concentration exceeds the DMSO solubility of the batch of drug.

Method for preparing in vivo formulation:Take μL DMSO stock solution, next add μL PEG300, mix and clarify, next addμL Tween 80, mix and clarify, next add μL ddH2O,mix and clarify.

(1) Please be sure that the solution is clear before the addition of next solvent. Dissolution methods like vortex, ultrasound or warming and heat may be used to aid dissolving.
             (2) Be sure to add the solvent(s) in order.

Biological Data
  • Small molecule screen to identify regulators of cartilage hypertrophy and differentiation. (A) Schematic representation of the high throughput screen performed to identify putative small molecule regulators of chondrocyte differentiation state. Limb mesenchymal cells were isolated from E13.5 mouse embryos carrying a Col10a1-mCherry transgene. Compounds were considered positive hits if they reduced mCherry signal after induction with the prodifferentiation factor BMP-4. (B) Quantitation of top 75 positive hits. (C) Structure of regulator of cartilage growth and differentiation (RCGD) 423. (D) RCGD 423 decreases levels of RUNX2 and COL 10 protein in articular chondrocytes from osteoarthritic donors (n=3). DMEM, Dulbecco’s Modified Eagle Media; OA, osteoarthritis.[1].Drug-induced modulation of gp130 signalling prevents articular cartilage degeneration and promotes repair. Ann Rheum Dis. 2018 May;77(5):760-769.
  • IL-6 family cytokines induce proinflammatory, catabolic signalling that can be directly competed by regulator of cartilage growth and differentiation (RCGD) 423. (A) Schematic of the proinflammatory signalling pathways that cause cell hypertrophy and matrix degradation in chondrocytes. (B) Adult pig articular chondrocytes were cultured for 24 hours with the indicated cytokines or RCGD 423 and the levels of pSTAT3 and MYC were quantified (C; n=3) with respect to histone H3. Representative data for other proteins in MAPK (p38 and pERK1/2), AKT (phospho-AKT; pAKT) or NF-κB (pNF-κB) are also shown. (D) Transcription of catabolic genes was determined via qPCR in adult pig articular chondrocytes treated with oncostatin M (OSM), IL-6, TNF-α, leukaemia inhibitory factor (LIF) or RCGD 423. Data are represented at mean±SD. (E) Adult human chondrocytes were incubated with the indicated cytokines in the presence or absence of RCGD 423 and the levels of downstream proteins quantitated with respect to histone H3. (F) Pig articular cartilage explants were incubated with OSM, RCGD 423 or both; levels of cleaved aggrecan and collagen epitopes in the supernatant are normalised to the wet weight of the explant. For all panels, n=3.[1].Drug-induced modulation of gp130 signalling prevents articular cartilage degeneration and promotes repair. Ann Rheum Dis. 2018 May;77(5):760-769.
  • Regulator of cartilage growth and differentiation (RCGD) 423 inhibits apoptosis and promotes proliferation via induction of pSTAT3 and MYC in adult human chondrocytes. (A) Adult human articular chondrocytes were incubated with or without RCGD 423 and levels of MYC and pSTAT3 were quantified relative to histone H3 after 24 hours. (B) Increases in pSTAT3 and MYC proteins occurred in both a dose-dependent and time-dependent fashion following stimulation with RCGD 423. (C) Single human adult articular chondrocytes were cultured for 5 weeks with or without stimulation with RCGD 423 and assessed for colony formation. (D) Adult human articular chondrocytes were incubated with or without RCGD 423 in Mebiol hydrogel for 24 hours and then apoptotic cells were quantitated via flow cytometry for annexin V. (E) Proliferation in explants of adult pig articular cartilage in the absence or presence of RCGD 423 as shown by EdU incorporation. Scale bars represent 25 μm. P<0.0001. n=5. [1].Drug-induced modulation of gp130 signalling prevents articular cartilage degeneration and promotes repair. Ann Rheum Dis. 2018 May;77(5):760-769.
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